Pathol Biol (Paris), 1989 Dec, 37(10), 1090 - 3 {Inhibition by nifurzide of the adhesion capacity of enteropathogenic colibacillus to HEP-2 cells}; Darfeuille-Michaud A et al.; Enteropathogenic Escherichia coli (EPEC) adhere in vivo to enterocytes . This adhesion capacity can be obtained in vitro with Hep-2 cells on which a characteristic localized adherence (LA) is observed . We studied the effect of subinhibitory concentrations (SIC) of nifurzide, a nitrofurane derivative, on this bacterial adherence phenomenon . Three EPEC strains are used: 11201 (026 serogroup), 7958 (0128) and 7836 (0142) . Various SIC (MIC/2; MIC/4;...; MIC/32) were added either to the culture medium of bacteria or to the Eagle medium in which bacteria and Hep-2 cells were mixed during the adhesion experiments . In each case an adhesion index is determined . Nifurzide strongly inhibits the adherence capacity of the three strains when concentrations ranging from MIC/2 to MIC/16 where added in both culture media . On the other hand three other nitrofurane derivatives which have no antibacterial effect did not inhibit adherence . The mechanism of the adherence inhibition by nifurzide is discussed. Vet Clin North Am Equine Pract, 1989 Dec, 5(3), 513 - 38 Equine bandaging techniques; Lindsay WA; Topical medications and bandages play an important role in the management of equine wounds . Certain water-soluble antibacterial ointments (povidone-iodine, polymixin-neosporin-bacitracin) may be appropriate for use on contaminated wounds . A well-designed equine bandage is usually composed of primary, secondary, and tertiary layers . Because so many different products are available, the practitioner is advised to become familiar with the handling characteristics of a few . Because of the irregular contours of the equine limb, only products that stretch and conform should be used . Bandages should be applied snugly and secured in such a fashion that they will not slip or ride up . The horse should be confined to a stall while bandaged, and, even then, bandages must be changed at frequent intervals. Semin Oncol, 1989 Dec, 16(6), 543 - 60 Infectious emergencies in oncology patients; Lazarus HM et al.; The development of neutropenia in a patient undergoing therapy for cancer represents a serious medical problem that rapidly escalates if fever develops . A diligent history and physical examination cannot be overemphasized, since this maneuver may direct the medical person to quickly identify the source of the infection and initiate appropriate therapy . No time should be wasted, but every attempt should be made to quickly obtain body fluids or tissue for microbiologic culture purposes . Appropriate therapy should then be instituted in an empiric manner . The antibacterial agents that are chosen as initial therapy should be selected based on a knowledge of the current local ecology and the antibiotic resistances of endemic strains of bacteria . The empiric therapy should continue until the patient has evidence of recovery of bone marrow function . In those patients who have developed obvious tissue infection, such as pneumonia or bloodstream infection, the therapy should be continued until the infection is eradicated . In patients who have persistent fever despite broad-spectrum antibacterial agents, a painstaking search for the source and type of infection should continue, including repeated blood cultures and other tests . Additional antibiotic or fungal agents should be administered as the need arises . Such an approach to this group of patients has resulted in a significantly better outcome for cancer patients . With the advent of recombinant hematopoietic growth factors, which may allow for a more rapid marrow and immunologic recovery, the therapy for the neutropenic patient should continue to improve. Pharmazie, 1989 Dec, 44(12), 817 - 20 {Azoles . 27 . Nitroimidazole derivatives, their antibacterial and fungicidal activity and electron affinity}; Zaprutko L et al.; Nitroimidazole derivatives 3a-3g, 4a-4g and 5-8 were synthesized by treating 4,5-dinitro- and 2-methyl-4,5-dinitroimidazole (1,2) with phenacyl bromide, its p-substituted derivatives or epichlorohydrin . 1-(3-Chloro-2-hydroxypropyl)-4,5-dinitroimidazole (5) and its 2-methyl derivative 6 have been converted to imidazo-oxazoles 7 and 8 or amino imidazole derivatives 9-14 by the action of potassium carbonate or cyclic amines (pyrrolidine, piperidine, morpholine and N-methylpiperazine) . Some of the newly synthesized nitroimidazole derivatives show antibacterial and fungicidal activity . The electron affinity of the nitroimidazole derivatives 1-24 is discussed on the basis of their half-wave potentials and in the connection with their eventual radiosensitizing properties. Akush Ginekol (Mosk), 1989 Dec, (12), 36 - 8 {The treatment of pregnant women with pyelonephritis}; Arbuliev MG et al.; Results of combined therapy comprising laser treatment of acupuncture sites, venous blood and the renal pelvic mucosa approached through a nephrostomy drain and ureteral catheter have been analyzed in 80 pregnant women with pyelonephritis . Laser treatment supported by antibacterial, fluid, spasmolytic, antihypertensive and immunostimulator therapy proved to be an effective regimen. J Antibiot (Tokyo), 1989 Dec, 42(12), 1817 - 22 Erythromycin A oxime 11,12-carbonate and its oxime ethers; Brain EG et al.; Erythromycin A oxime 11,12-carbonate (5a) and its oxime ethers 5b approximately 5p have been prepared and their antibacterial activities compared with those of erythromycin A (1) and its 11,12-carbonate 2 . The oxime 5a and many of its oxime ether derivatives showed good activity in vitro against Gram-positive and the more permeable Gram-negative organisms, in some cases being even more active than the carbonate 2. J Chemother, 1989 Dec, 1(6), 369 - 73 Effect of slime production on the antibiotic susceptibility of isolates from prosthetic infections; Selan L et al.; The antibacterial activity of 6 antibiotics towards 10 gram-positive and 6 gram-negative glycocalyx-producing strains, has been evaluated by employing a method which partially simulates the in vivo colonization of prosthetic devices . The results showed that routine antibiotic sensitivity tests are not predictive about the response of the glycocalyx-embedded bacteria, and that prophylaxis may be useful with ofloxacin and clindamycin, before placing a prosthetic device . Once bacterial colonization had already occurred, however, none of the tested antibiotics was able to eradicate the sessile bacterial form . The minimum bactericidal concentration (MBC) values, indeed, were much higher than those determined on the planktonic form, and were much higher than serum and tissue levels that can be reached in vivo. Acta Odontol Scand, 1989 Dec, 47(6), 361 - 6 The effect of chlorhexidine supplementation in a periodontal dressing; Othman S et al.; Most commercial periodontal dressings claiming antibacterial activity lose this activity shortly after application . Chlorhexidine (CH) is an antibacterial agent with long-term activity in the oral cavity owing to its substantiveness and slow-release properties . In a double-blind split-mouth-designed clinical trial the effect of incorporating CH acetate in periodontal dressing was tested on wound healing after gingivectomy . Eleven patients, each needing at least two gingivectomies, constituted the test panel . Wound healing, as assessed by bleeding tendency after removal of dressing 7 days postoperatively was significantly delayed when control dressings were applied as compared with test dressings . Variables with regard to patient comfort also yielded results in favor of the test pack . Incorporation of antibacterial agents with high retention and slow release properties in the mouth in surgical dressings seems advantageous. Presse Med, 1989 Nov 25, 18(39), 1923 - 7 {Structure-activity relationship of oral cephalosporins}; Bingen E et al.; The advances achieved in the field of oral cephalosporins consist of improved bioavailability and enhanced intrinsic activity of the compounds . Oral absorption is facilitated either by creating prodrugs or by modifying the compound itself with addition of the alpha-amino group at position 7 on the cephem ring or of a vinyl group at position 3 . Antibacterial activity and resistance to beta-lactamases are facilitated by the presence of an amino-2-thiazole heterocycle at position 7, associated with a methoxy-imino group or an oxy-imino-acetoxy group. Methods Find Exp Clin Pharmacol, 1989 Nov, 11(11), 697 - 701 Lack of cross-resistance between efrotomycin and antibacterial agents used in the therapy of human and animal infections; Jacks TM et al.; Efrotomycin is an N-methylhydroxypyridone glycoside antibiotic with activity primarily against Gram-positive bacteria . It is intended for use as a feed additive for swine . Although efrotomycin is unrelated to any antibacterial drug used in human or veterinary medicine, the possibility of cross-resistance with other antibacterials is of concern . The minimum inhibitory concentrations (MICs) of efrotomycin were determined for a broad panel of bacterial isolates . In addition, the susceptibility of each isolate to 12-15 antibacterials was determined using a standardized disk susceptibility test . No evidence of cross-resistance between efrotomycin and any of the 12-15 antibacterial compounds was observed . When the MIC of efrotomycin for nine selected isolates was increased from 16- to greater than 100-fold by serial passage in subinhibitory concentrations of efrotomycin, no increased resistance to the 15 antibacterials was noted . Subinhibitory concentrations of efrotomycin had no effect on the conjugative transfer of antibacterial-resistance plasmids between K-12 strains of Escherichia coli . The data from this study suggest that if resistance to efrotomycin should occur, it is unlikely to result in the appearance of multiply-resistant bacterial populations. Jpn J Antibiot, 1989 Nov, 42(11), 2354 - 62 {In vitro susceptibility of pathogenic Nocardia to beta-lactam antibiotics, especially imipenem, a carbapenem antibiotic}; Yazawa K et al.; In vitro antibacterial activity of 30 beta-lactam antibiotics including 2 beta-lactamase inhibitors (clavulanic acid and sulbactam) against 2 major pathogenic Nocardia, i.e . Nocardia asteroides group and Nocardia brasiliensis was studied . Among the antibiotics tested, a newly developed carbapenem antibiotic, imipenem (IPM), was found to be the most active, followed by oxacephem group antibiotic flomoxef (FMOX) . IPM exhibited activity against only N . asteroides group (N . asteroides, Nocardia farcinica and Nocardia nova) . On the other hand, FMOX showed activity against all pathogenic Nocardia tested . A 2- to 30-fold decreases in minimum inhibitory concentration (MIC) for N . asteroides, N . brasiliensis and N . farcinica was noted when antibiotics and beta-lactamase inhibitors were combined compared to antibiotics alone . Further combination and enzymatic studies indicated that all pathogenic Nocardia possess beta-lactamase except for a half of the strains of N . nova . These species' specific sensitivity patterns of pathogenic Nocardia are discussed in this paper with references to their taxonomic positions. J Clin Periodontol, 1989 Nov, 16(10), 630 - 5 Efficacy of Perimed antibacterial system on established gingivitis . (I) . Clinical results; Clark WB et al.; A 6-month, double-blind controlled study was conducted on 101 subjects to determine the effect of Perimed antibacterial system, containing povidone-iodine (PVP-I) and hydrogen peroxide (H2O2), on established gingivitis . Subjects were randomly assigned to one of 4 treatment groups: PVP-I/H2O2, PVP-I/H2O, H2O2/H2O or H2O . Gingivitis was assessed by the papillary bleeding score (PBS) and plaque by a modified Quigley-Hein plaque index (PI) at baseline, 3, 12 and 24 weeks . The average baseline PBS and PI for the 4 groups ranged from 2.16-2.31 and 2.87-2.90, respectively . After baseline evaluation, subjects received a supra-gingival scaling and a subgingival irrigation with their respective rinse . Daily rinses were supervised and subgingival irrigation was repeated every 3 weeks . Duncan's multiple range test determined which groups differed from each other . The mean PI at 24 weeks was lower than at baseline in all groups . PVP-I had the lowest PI at all time points . The mean PBS at 24 weeks was 1.48 for PVP-I, 1.62 for H2O2, 1.88 for H2O and 1.34 for PVP-I/H2O2, a reduction from baseline of 31%, 27%, 18%, and 38% respectively . The difference between the PBS for PVP-I/H2O2 and H2O control was significant at each evaluation . There was a 70% reduction in sites with PBS greater than or equal to 3 for PVP-I/H2O2 between baseline and 24 weeks compared to a 34% decrease in the H2O group . It was concluded that the use of Perimed could be a beneficial adjunctive treatment for the prevention and control of gingivitis when used with routine oral hygiene procedures. Rev Infect Dis, 1989 Nov-Dec, 11 Suppl 7, S1572 - 81 Antibiotic therapy for the febrile granulocytopenic cancer patient: combination therapy vs . monotherapy; Wade JC; The specific composition of empiric antibiotic therapy to be implemented for patients with neutropenia and fever remains controversial . The available clinical data comparing antibiotic combination with monotherapy come from studies with a number of major differences in design and analysis that make it difficult to interpret relative efficacy . The standard practice has been to use an antibiotic combination demonstrating broad antibacterial coverage, additive or synergistic effects against the more virulent gram-negative pathogens, and potentially antibacterial activity that decreases the emergence of resistant organisms . Studies of monotherapy have been hindered by wide differences in study design, and few comparative data have been presented to substantiate the efficacy of the drug in question as "treatment of infection"--an exception being the new agent imipenem . The emergence of gram-positive organisms as frequent pathogens in neutropenic patients has raised concern regarding empiric gram-positive therapy . Clinical experience suggests that empiric therapy is unnecessary; rather, directed therapy with an agent such as vancomycin can be used in those situations in which clinical or microbiologic data suggest the need for such antibiotics . If the specifics of optimal management of infectious disease in patients with sustained neutropenia and fever are to be identified, many continuing clinical problems must be approached in a more systematic and defined manner . Defects in study designs of the past should be eliminated, with investigators taking a stronger stand in support of standardized design and analysis. J Antimicrob Chemother, 1989 Nov, 24(5), 765 - 74 In-vivo and in-vitro interference of antibiotics with antigen-specific antibody responses: effect of josamycin; Villa ML et al.; The effects of josamycin on the antigen-specific primary antibody responses of human peripheral blood cells have been studied by the method of haemolytic colonies in soft agar . The tests were performed before and after the oral administration of 1 g of josamycin or by adding the drug directly to cultures of cells from untreated donors . The results demonstrate that josamycin, added in vitro or administered in vivo significantly depresses the primary antibody responses . The mechanism by which josamycin exerts its activity on antibody production has been partially elucidated . The immunodepression depends on the stimulation of hydrogen peroxide production by monocytes and requires the actual presence of josamycin during the immune response . The stimulation of the respiratory burst of the phagocytic cell is a common feature of macrolide antibiotics and suggests the need for more extensive clinical and preclinical trials on antibacterial antibiotics that alter the human immune responses. Am Ind Hyg Assoc J, 1989 Nov, 50(11), 579 - 85 Hexamethylenetetramine: a review; Dreyfors JM et al.; The available literature on hexamethylenetetramine (hexamine) was reviewed with emphasis on its toxicology and epidemiology, its thermal decomposition and regulatory concerns related to its uses . Large quantities of hexamine are used in the foundry, tire and rubber, and phenolformaldehyde resins industries and in other diverse applications . Excessive exposure to solid hexamine or its vapor has been reported to cause dermatitis and respiratory allergies . Although hexamine produces a positive Ames test, most animal studies have shown hexamine to be of very low genetic risk even in very high doses . The effectiveness of hexamine as an antibacterial agent has been attributed to its slow hydrolysis to ammonia and formaldehyde . Concerns have developed in industries which use hexamine at high temperatures over emissions of HCN, NH3, CO, CO2, nitrogen oxides, and formaldehyde . The studies reviewed are in general agreement that hexamine thermal decomposition in the temperature range of 300-800 degrees C is characterized by an increase in HCN and a decrease in NH3 emissions with increasing temperature . At temperatures of 200-300 degrees C hexamine decomposition is reported to produce mainly ammonia and formaldehyde. ZWR, 1989 Nov, 98(11), 962, 964 - 5 {Bactericidal effects of antiseptic gypsum}; Lotzmann U et al.; In tests with plaster models we inspected the antibacterial effect of the dental plasters Dento-rock and Dento-dur . The results show, that models consisting of plaster that contains Chloramin T 80 were free of bacteria, even when produced from bacterial contaminated alginate impressions . After separation of the plaster models from the alginate impressions, a bactericide effect could be traced to a layer of 220 microns below the surface of the alginate . By using dental plaster of the tested types, it is therefore possible to eliminate the risk of a bacterial infection through plaster models, without any extra investing in time or labor . There is no sign of a negative influence of chloramin on physical parameters of the tested plasters. Chem Pharm Bull (Tokyo), 1989 Nov, 37(11), 3050 - 3 Biopolymers from marine invertebrates . X . Mode of action of an antibacterial glycoprotein, aplysianin E, from eggs of a sea hare, Aplysia kurodai; Kisugi J et al.; An antibacterial factor, aplysianin E, was purified from the eggs of a sea hare, Aplysia kurodai . Purified aplysianin E was a glycoprotein of 250 kilo daltons consisting of 3 subunits, and showed both antibacterial and antineoplastic activities . The two activities were lost in parallel on heating and at low and high pH . This factor was half-maximally active for gram-positive and -negative bacteria at 0.12-3.3 micrograms/ml and its action was not bactericidal but bacteriostatic . Aplysianin E did not induce morphological elongation of bacteria or their release of adenosine triphosphate (ATP), but it completely inhibited the syntheses of deoxyribonucleic acid (DNA) and ribonucleic acid (RNA) by E . coli within 10 min . These results suggest that aplysianin E, found in an invertebrate, the sea hare, is a new antibacterial protein and that it exerts its action by inhibiting nucleic acid synthesis, as a DNA-inhibiting chemotherapeutic drug does. Arch Pharm (Weinheim), 1989 Nov, 322(11), 821 - 6 {Peroxides as plant constituents . 6 . Hydroperoxides from the blossoms of Roman camomile, Anthemis nobilis L}; Rucker G et al.; From the ethanol extract of the blossoms of Anthemis nobilis L . (syn . Chamaemelum nobile L.), six new hydroperoxides (1-6) were isolated, besides the known 1 beta-hydroperoxyisonobilin (7) . The structures were elucidated by spectroscopic methods and in some cases ascertained by synthesis . Compounds 2 and 3 show a medium antibacterial activity. Stomatologiia (Mosk), 1989 Nov-Dec, 68(6), 10 - 1 {The use of the preparation baliz-2 in inflammatory processes of the maxillofacial area}; Bernadskaia GP et al.; Examinations of 137 patients with inflammatory diseases of the maxillofacial area and neck, treated with baliz-2, have shown that this agent is characterized by a manifest antibacterial action on the wound microflora, helps thinning the purulent exudate, and accelerates detachment of the necrotic mass . No cases of local irritation were recorded. Arzneimittelforschung, 1989 Nov, 39(11), 1406 - 10 Synthesis, antibacterial activity and structure-activity relationships of N-substituted 3-methyl-4-diazo-5-pyrazolecarboxamides; Baraldi PG et al.; A number of N-substituted 3-methyl-4-diazo-5-pyrazolecarboxamides (IVa-p) have been synthesized and tested for their in vitro antibacterial activity . All the compounds have been assayed against several representative Gram-negative and Gram-positive bacteria, as well as against some intestinal bacterial species . Some of the 4-diazopyrazoles IVa-c have shown a quite interesting broad-spectrum activity, while they are ineffective against the "protective" intestinal flora . The structure-activity relationships of the series have been studied quantitatively, via both univariate and multivariate methods: the results are consistent and permit some rationalization of the behaviour of the compounds investigated. Cardiovasc Res, 1989 Nov, 23(11), 960 - 4 Effects of antibiotics on cellular viability in porcine heart valve tissue; Hu JF et al.; The purpose of this study was to find an antibiotic disinfecting solution for cardiovascular tissues which would allow maximal cellular viability while maintaining antibacterial and antifungal activity . Cellular viability of porcine heat valves sterilised using antibiotics was assessed by radiolabelled proline transport assays . The results show that storage of valve tissues in RPMI 1640 tissue culture medium (4 degrees C) alone decreases the cellular viability by 50%, 60% and 90% within 12, 24, and 72 h, respectively . Amphotericin B was shown to be the toxic component of the antibiotic sterilising solution recommended by Strickett and coworkers, accounting for all the observed antibiotic toxicity . It reduced the cellular viability by 100% within 12 h of storage at 4 degrees C . Our study also showed that streptomycin is responsible for the loss of cellular viability in the antibiotic medium utilised by O'Brien's group . The results show that after storage of valve tissues for 12 h in O'Brien's antibiotic solution, the cellular viability was reduced by 60%, and after 24 h by 90% . Cefoxitin, lincomycin, polymyxin B, vancomycin and penicillin had no apparent effects on viability of cells in the cardiovascular tissues utilised in this study . In conclusion, heart valve tissue may be sterilised effectively using selective antibiotics without causing significant damage to cellular viability. Z Gesamte Inn Med, 1989 Nov 1, 44(21), 658 - 60 {Lyme borreliosis with erythema chronicum migrans and Garin-Bujadoux-Bannwarth meningopolyneuritis}; Berthold F et al.; A case report is given on a Borrelia burgdorferi infection regarded to be typical because of its clinical course and the diagnosis lately made . The meningopolyneuritis was treated by use of corticosteroids before the serologic detection of Lyme disease . 21 months after infection our patient died of a colon carcinoma . Histological preparation of the brain showed a slight encephalitis we consider as third-stage Lyme borreliosis . We conclude that antibacterial therapy is necessary in the management of Lyme disease, especially after the administration of corticosteroids. Pharmacol Biochem Behav, 1989 Nov, 34(3), 649 - 53 D-cycloserine, a positive modulator of the N-methyl-D-aspartate receptor, enhances performance of learning tasks in rats; Monahan JB et al.; Glycine has recently been shown to positively modulate the N-methyl-D-aspartate (NMDA) subclass of acidic amino acid receptors which are important in neural pathways involved in learning and memory . We report that d-cycloserine (DCS), an antimycobacterial agent known to cross the blood-brain barrier, binds with high affinity to this glycine modulatory site, functions as a positive modulator, and facilitates performance of learning tasks in rats . In addition, DCS appears to be a potent cognitive enhancer at doses lower than those required for antibacterial activity . Based on these data, we propose that modulation of NMDA receptors via glycinergic mechanisms may be a means of influencing cognitive processes. J Antibiot (Tokyo), 1989 Nov, 42(11), 1684 - 97 Dechloro teicoplanin antibiotics; Malabarba A et al.; Mono- and didechlorinated derivatives of the antibiotic teicoplanin, its pseudoaglycones and aglycone, and of one amide and ester of deglucoteicoplanin were prepared under selective reductive conditions . The selectivity and rate of dehalogenation were studied and compared to those of vancomycin and deglucovancomycin . The influence of the chlorine substituents on the mechanism of action and antibacterial activity of teicoplanin antibiotics was also investigated. Vrach Delo, 1989 Nov, (11), 39 - 40 {The optimization of the corticosteroid therapy of patients with destructive pulmonary tuberculosis}; Iareshko AG; Corticosteroids were administered in 120 patients with active pulmonary tuberculosis during the morning hours every other day in association with tuberculostatic agents . It was found that corticosteroids in a dose similar to 15 mg of prednisolone did not influence the efficacy of antibacterial agents while an increase to 20 mg used for not less than 2 months increases the treatment efficacy to 83.3% and over 3 months--to 89.5%. Klin Med (Mosk), 1989 Nov, 67(11), 81 - 5 {The role of disorders of secretion of pancreatic enzymes and bile and bacterial contamination of the small intestine in the pathogenesis of diarrhea in patients with celiac disease}; Loginov AS et al.; The study of 53 patients with celiac disease provided evidence for the impotent role of the inhibited hyposecretion of pancreatic enzymes, atony of the gallbladder responsible for abnormal bile acids introduction into the intestinal lumen in digestion, elevated concentrations of free bile acids at the expense of lowjugated ones in duodenal and jejunal contents as well as bacterial dissemination of the proximal portion of the small intestine in pathogenesis of diarrhea observed in celiac disease . It is concluded that inclusion of continuous courses of enzyme preparations and light cholagogues in the treatment schemes of celiac disease and administration in its exacerbation of adsorbents, astringents, antibacterial preparations should be necessary therapeutic measures. Biochim Biophys Acta, 1989 Oct 2, 985(1), 60 - 6 The lipopeptide antibiotic A21978C has a specific interaction with DMPC only in the presence of calcium ions; Lakey JH et al.; The A21978C group are lipopeptide antibiotics which kill Gram-positive bacteria only in the presence of calcium ions . The calcium requirement of the antibacterial activity of A21978C correlates well with an in vitro calcium-dependent insertion into phospholipid vesicles . In this paper the interaction of A21978C with phosphatidylcholine is investigated in mixed monomolecular films . The spontaneity of the antibiotic-lipid mixing was determined by calculating the free energy change . On a Ca2+ containing subphase there is a specific interaction between the components at all antibiotic-lipid ratios . This is not true on K+ subphases, where specific interactions never occur . On Mg2+ subphases specific interactions occur only in monolayers containing very little lipid . By analysing the fluorescence of the kynurenine residue we have followed the effects of two factors on the penetration of the antibiotic into lipid bilayer vesicles . Firstly, the phospholipid gel to liquid crystalline phase transition which in the absence of calcium leads to an exclusion of the antibiotic from the bilayer . This trend is completely reversed in the presence of Ca2+ . Secondly, the role of this lipopeptide's lipid tail was clarified by use of a series of versions of increasing fatty acyl chain length . The results indicate that the interaction promoted by calcium is not simply a hydrophobic attraction between fatty acyl chains but is more likely to be a specific interaction between polar headgroups. J Antibiot (Tokyo), 1989 Oct, 42(10), 1489 - 93 LL-E19020 alpha and beta, animal growth promoting antibiotics: taxonomy, fermentation and biological activity; Maiese WM et al.; Antibacterial antibiotics LL-E19020 alpha and beta were isolated from the fermentation broth of an actinomycete strain . Based on cultural and physiological characteristics, culture LL-E19020 was identified as a new subspecies of Streptomyces lydicus . The LL-E19020 alpha and beta antibiotics were found to possess a very narrow antibacterial spectrum against human pathogens . In studies in chickens, LL-E19020 alpha demonstrated excellent growth promoting activity. Am J Med Sci, 1989 Oct, 298(4), 252 - 5 Subacute disseminated mucormycosis in a diabetic male; Nolan RL et al.; Mucormycosis is an opportunistic invasive infection caused by fungi of the order Mucorales . Rhizopus, Absidia, and Mucor are the most commonly encountered genera . Disease is characterized by vascular invasion, thrombosis, and tissue necrosis . Rhinocerebral disease is the most common manifestation but pulmonary, cutaneous, gastrointestinal, and widely disseminated forms have been reported . Pulmonary and disseminated disease are usually seen in neutropenic patients with leukemia or lymphoma . Both present as fever and unexplained pulmonary infiltrates unresponsive to antibacterials and corticosteroids . Disease is usually fulminant and has a high mortality rate . Diagnosis is most commonly made at autopsy . A single case of disseminated disease is reported that is unusual in its subacute course and its occurrence in an otherwise healthy non-neutropenic diabetic male. Dig Dis Sci, 1989 Oct, 34(10), 1576 - 80 Cholestatic hepatitis due to antibacterial combination of amoxicillin and clavulanic acid (augmentin) Stricker BH, Van den Broek JW, Keuning J, Eberhardt W, Houben HG, Johnson M, Blok AP. Five case histories are presented of patients developing cholestatic hepatitis associated with the intake of the antibiotic combination agent amoxicillin and clavulanic acid (Augmentin) . In two of these cases, signs of hepatic injury recurred after readministration of this combination but not after the intake of amoxicillin alone . In none of the patients was another cause for cholestatic hepatitis found and extrahepatic causes were excluded by ultrasonography, CT scanning, or ERCP . Most viral causes of hepatic injury were excluded in these patients . With the exception of one patient, who developed a transient rash, no immunoallergic signs were present . Biopsy in two patients showed extensive cholestasis without significant necrosis . Clavulanic acid seems to be responsible for this adverse effect. Minerva Pediatr, 1989 Oct, 41(10), 515 - 20 {Clinical evaluation of letosteine activity in the treatment of acute febrile bronchitis in children . Double-blind controlled study versus placebo}; Nespoli L et al.; A double blind vs placebo study was carried out to study the effect of letosteine on the symptoms and clinical course of paediatric patients suffering from acute febrile bronchitis . Forty children were recruited for the research: 20 were treated with letosteine in a dose of 25 mg x 3 g/die and 20 with placebo; treatment lasted 10 days . The following parameters were assessed during the trial: body temperature, cough, thoracic objectivity, respiratory function indices . The results of the study show that in the letosteine treated group there is a statistically significant decrease in fever, a favourable evolution of thoracic objectivity and an improvement in certain respiratory function parameters (MEF 75, PEF) . It is concluded that treatment with letosteine leads to a significant increase in the rate of regression of thoracic symptomatology and a faster, more substantial reduction in fever in children suffering from acute bronchitis . This is probably the result of drug action on mucus viscosity, restoring optimal mucociliary clearance, and through action fostering the penetration of antibacterial substances into the mucus. Am J Infect Control, 1989 Oct, 17(5), 258 - 63 Evaluation of the insulin jet injector as a potential source of infection; Price JP et al.; In recent years jet injection of insulin has been widely used by patients with diabetes mellitus . Jet injectors may become contaminated by bacteria because of repeated use without cleaning; cleansing every 2 weeks is recommended . We investigated the occurrence of bacterial contamination by culturing jet injectors in everyday use by 19 patients with diabetes . Swabs from the interior chambers were cultured on blood agar plates . Only one of 20 cultures yielded bacterial growth, and the organism recovered was a presumed contaminant that could not be identified as any common pathogen . No study patient, nor any of more than 70 patients whom we instructed in jet injection, showed any clinical evidence of infection attributable to jet injector use . Jet injectors are unlikely to become colonized by bacteria or to cause infection in patients using them for insulin administration . The low rate of colonization may be due to the antibacterial preservatives added to commercial preparations of insulin . Additional data based on larger numbers of patients would be useful in further clarifying the risk of infection associated with jet injectors. J Anim Sci, 1989 Oct, 67(10), 2817 - 21 Sulfa residues in pork: an update; Augsburg JK; Sulfamethazine (SMZ) is an antibacterial drug used in approximately 75% of all hogs marketed in the U.S . The tolerance for residues of SMZ in uncooked tissues is .1 ppm, and the withdrawal time is 15 d . The rate of illegal residues in swine from the use of SMZ has continued to fluctuate between 4% and 5% from 1980 through 1987 . This was not acceptable . The Center for Veterinary Medicine (CVM) also has received from the National Center for Toxicological Research a report showing that SMZ produces a dose-related increase in follicular cell adenomas of the thyroid gland in rats and mice . The FDA has discovered three major causes of SMZ residues by investigating violators . The number one cause was a lack of sequencing, flushing, and cleaning of mixer equipment . Failure to follow withdrawal times was another major cause, and the third major reason was the use of a soluble powder solution . At least 16% of SMZ residue violations have resulted in no follow-up due to lack of animal identification . The FDA district offices are conducting on-farm investigations of swine producers who have caused SMZ violations . Repeat violators and those that produce higher residue levels will receive a higher priority . The FDA currently is attempting to obtain more state support, particularly for investigation of first-time violators . The CVM is serious about resolving the SMZ residue problem. Endod Dent Traumatol, 1989 Oct, 5(5), 242 - 52 Pulpal response to an anhydrous glass ionomer luting cement; Tobias RS et al.; This investigation was designed to study the pulpal responses to Aquacem, an anhydrous glass ionomer luting cement, and to compare the results with those previously obtained for a conventional glass ionomer luting cement, Chembond . The study was carried out according to the BSI (1980) recommendations for testing restorative materials in vivo . Aquacem caused more pulpal inflammation than the control material, Kalzinol, though by an indirect mechanism . The statistical model demonstrated a significant association between bacterial presence within the experimental cavity and pulpal inflammation . The type of restorative material has no direct association with the degree of inflammation, but the model suggests that it exerts an indirect influence via its antibacterial properties and hence its influence on microbial microleakage. Antibiot Khimioter, 1989 Oct, 34(10), 779 - 82 {Comparative evaluation of the embryotoxic effect of various antibiotics}; Skosyreva AM; A broad spectrum of antibacterial antibiotics used in treatment of purulent inflammatory diseases in pregnant women was studied experimentally . The antibiotics included oxacillin, fusidin, kanamycin, gentamicin, cefuroxime, cephalothin and tetracycline . The embryotoxic action of the antibiotics was investigated on embryos of rats cultivated in vitro . The mediated antenatal action of tetracycline and gentamicin was studied during various gestation terms before implantation (days 1 to 7), during organogenesis (days 8 to 14) and during fetal growth++ (days 14 to 20) . Prior to the delivery the data on the intrauterine death, development of the fetoplacental unit and the presence of external and internal anomalies were considered . The placenta, liver and kidneys of the fetus were examined morphologically . It was shown that tetracycline and gentamicin had embryotoxic properties as evidenced by a higher intrauterine death rate and congenital anomalies in individual fetuses. Minerva Cardioangiol, 1989 Oct, 37(10), 443 - 9 {Surgical cardiac risk in patients with heart diseases . II . Perioperative treatment}; Caruzzo C et al.; An improvement can be obtained in the surgical prognosis of the cardiopathic by working on the main risk factors . Congestive decompensation must usually be treated with diuretics; digitalis in only indicated in certain cases . In patients with ischaemic cardiopathy, angina therapy should be continued during the perioperative period, replacing the oral route; in the postoperative period . ECG monitoring is advisable up to Day III-V . Valve defects should be assessed carefully, including haemodynamically (especially severe aortic stenosis) because correction of the defect may become a priority . In hypertrophic cardiomyopathy hypovolaemia and loss of sinus rhythm should be avoided . Valve prostheses involve particular problems represented by antibacterial prophylaxis and perioperative anti-coagulation . Congenital cyanogenic cardiopathies often require a lowering of the haematocrit and careful control of hypotension . Postoperative arrhythmias generally have medical causes and require control of the latter before possible antiarrhythmic therapy . The implantation of a temporary prophylactic pacemaker is rarely needed; for patients with definitive pacemakers, some precautions are needed for the use of the thermocautery . It is very important to deal with poor general medical conditions that might affect prognosis . Control of hypertension is less important than control of hypotension. Int J Pept Protein Res, 1989 Oct, 34(4), 277 - 86 A common cytolytic region in myotoxins, hemolysins, cardiotoxins and antibacterial peptides; Kini RM et al.; Several proteins and polypeptides of reptilian, amphibian, insect, and microbial origin share a common cytolytic property . However, these cytolysins fulfill different objectives . They provide offensive armament in the case of toxins, but defensive systems in the case of antibacterial peptides . The sequences of several nonenzymatic cytolysins and their analogues were compared to identify the structural requirements for cytolytic activity . These cytolysins, although isolated from phylogenetically unrelated organisms, possess the common sequence features of a cationic site flanked by a hydrophobic surface . The presence of such a region apparently confers the cytolytic activity of various cytolysins . The concept of a cytolytic region is strongly supported by the existence of several natural and synthetic analogues of cytolysins and by chemical modification studies of these cytolysins . This prediction provides a new focus for cytolysin research . The understanding of this structure-function relationship should facilitate the design, synthesis, and development of better antibacterial and anticancer peptides. Microbiologica, 1989 Oct, 12(4), 307 - 16 Antibacterial, antifungal and antitumoral activities of Micromycetes . I . Preliminary study; Steiman R et al.; The ability of 211 strains of Micromycetes to produce antibiotic, antifungal and antitumoral compounds has been investigated in vitro using test strains and P 388 leukemia cells . Cytotoxicity was determined on Vero cells . Convenient activities were obtained depending on the taxonomic group . Finally, 17 strains of Micromycetes were selected for their antibacterial or antifungal activities and 12 for their antitumoral properties . Investigations are in progress concerning these activities. Arch Pharm (Weinheim), 1989 Oct, 322(10), 599 - 602 Synthesis and biological properties of novel triazolopyrimido-pyrimidine-5,8-diones; Dlugosz A; The synthesis of novel 1,2,4 triazolo{2,3,4-c,d}pyrimido{4,5-d}pyrimidine derivatives has been described from N-substituted amides of 1,2,3,4-tetrahydro-6-methyl-2-oxo-4-thio-5-pyrimidinecarboxylic acid 1 . Amides 1 treated with 80% hydrazine hydrate, followed by aqueous-ethanolic formaldehyde form substituted triazolo{4,3-c}pyrimidines which cyclize in pyridine to triazolopyrimidopyrimidine derivatives 4 . Attention has been paid to the synthesis of the 4-arylidenehydrazinopyrimidines 3 . Some compounds have been tested for antibacterial and anticancer activities and for action on CNS. Antimicrob Agents Chemother, 1989 Oct, 33(10), 1697 - 703 Use of in vitro topoisomerase II assays for studying quinolone antibacterial agents; Barrett JF et al.; Several quinolones and antitumor compounds were tested as inhibitors of purified calf thymus topoisomerase II in unknotting, catenation, radiolabeled DNA cleavage, and quantitative nonradiolabeled cleavage assays . The antitumor agents VP-16 (demethylepipodophyllotoxin ethylio-beta-D-glucoside) and ellipticine demonstrated drug-enhanced topoisomerase II DNA cleavage (the concentration of drug that induced 50% of the maximal DNA cleavage in the test system {CC50}) at levels of less than or equal to 5 micrograms/ml . Nalidixic acid, norfloxacin, and oxolinic acid did not induce significant topoisomerase II DNA cleavage, whereas ciprofloxacin did induce some cleavage above background levels . CP-67,015, a new 6,8-difluoro-7-pyridyl 4-quinolone which possesses potent antibacterial activity, inhibited bacterial DNA gyrase at 0.125 micrograms/ml in a nonradioactive DNA cleavage assay . Unlike other quinolones characterized to date, CP-67,015 was shown to strongly enhance topoisomerase II-induced radiolabeled DNA cleavage with a CC50 of 33 micrograms/ml and demonstrated cleavage in a nonradiolabeled DNA cleavage assay with a CC50 of 73 micrograms/ml . The topoisomerase II-mediated cleavage of DNA by CP-67,015 is consistent with its reported clastogenic effect on DNA in cell culture and its positive mutagenic response in mouse lymphoma cells . In vitro topoisomerase II catalytic and cleavage assays are useful for gaining preliminary information concerning the possible interaction(s) of some quinolones with eucaryotic topoisomerase II which may relate directly to their safety (mutagenicity, clastogenicity, or both) in human and veterinary medicinal usage. Akush Ginekol (Mosk), 1989 Oct, (10), 21 - 3 {Laparoscopic picture in patients with oligomenorrhea treated for chronic salpingo-oophoritis}; Gurtovaia NB et al.; Sixty patients with oligomenorrhea and the painful syndrome were examined to study the course of a chronic inflammatory process of the genitals . Laparoscopy has confirmed the initial diagnosis of salpingo-oophoritis in 24 of the 60 examinees . The authors call for a more thorough examination of this patient population, for an erroneous diagnosis of a chronic inflammation leads to erroneous therapeutic strategy, consisting in irrational administration of antibacterial, balneo- and physiotherapy. Immun Infekt, 1989 Oct, 17(5), 169 - 74 {The granulomatous inflammation in bacterial infections}; Kaufmann SH; The relevance of the granuloma to protection against intracellular pathogens has been recognized for a long time . More recently, it has become clear that the cell interactions which take place in a granuloma are highly complex . It appears that not only activation of antibacterial function in infected macrophages by helper T cells, but also lysis of infected host cells is of importance and that a coordinated interplay between different populations of T cells and mononuclear phagocytes is required for effective host resistance. Farmaco, 1989 Oct, 44(10), 997 - 1006 Biological studies on 1,2-benzisothiazole derivatives . II . Evaluation of antibacterial, antifungal and DNA-damaging activities of 3-amino, 3-acylamino, 3-alkylaminoacylamino derivatives; Zani F et al.; The in vitro evaluation of antibacterial, antifungal and DNA-damaging properties of some 3-amino, 3-acylamino and 3-alkylaminoacylamino derivatives of 1,2-benzisothiazole is described . Compounds 1-8, 38 and 48 exhibited a selective antifungal activity while the other compounds did not show any significative activity . None of the compounds tested turned out to have any genotoxic properties. Presse Med, 1989 Sep 30, 18(30), 1466 - 8 {Prompt antibiotic prophylaxis in resection of the prostate and removal of the bladder catheter}; Duclos JM et al.; Several regimens of antibiotic prophylaxis have been used in transurethral prostatic resection . In this study 50 patients received 1 g of cefotaxime during resection and thereafter were divided at random into two groups: one group received another 1 g dose of cefotaxime when the bladder catheter was removed, while the other group was left untreated at that stage . The administration of cefotaxime during both prostatic resection and catheter removal resulted in a highly significant reduction of infection risk, duration of hospitalisation and cost of antibacterial treatment . The most important risk of sepsis seems to be related to an apparently innocuous procedure: removal of the bladder catheter with resumption of spontaneous micturition. Tijdschr Diergeneeskd, 1989 Sep 15, 114(18), 939 - 48 {Escherichia coli mastitis in cattle . III . Antibacterial therapy}; Kremer WD et al.; This review paper is concerned with antibacterial therapy of mastitis caused by Escherichia coli . The choice of an antibacterial agent is discussed, and nine criteria are referred to, on which this choice should be based . In the second part possible forms of antibacterial treatment are discussed . Literature on parenteral and local treatment of mastitis due to E . coli is scarcely available . The evaluation of antibacterial drugs is mainly based on MIC values and pharmacokinetic studies in normal animals . Unfortunately, results of clinical trials are hardly available . Today combinations of trimethoprim/sulphonamide apparently are the best available choice for the parenteral treatment of mastitis caused by E . coli . Infusion of polymyxins or gentamycin is discussed as a method of intramammary therapy. Med J Aust, 1989 Sep 4, 151(5), 269 - 72 How well are endoscopes cleaned and disinfected between patients? Collignon P, Graham E. A questionnaire was sent to 276 hospitals throughout Australia to obtain details on the methods that are used in these institutions for the cleaning and disinfection of endoscopes . A broad range of hospitals was surveyed and 145 responses were received . Endoscopies were performed in 123 of the responding hospitals . Only 45% (55/123) of these hospitals both cleaned and disinfected their endoscopes satisfactorily . Generally, such hospitals were larger (300-600 beds) than were those which did not do so (100-300 beds) and also they were busier as more endoscopies were performed on a weekly basis (30.2 endoscopies compared with 19.3 endoscopies, respectively) . Frequently (38% {47/123} of hospitals), the endoscopes were not disinfected between patients, or were disinfected for an insufficient time or were disinfected with an agent that did not have both antiviral and antibacterial activity . In a substantial proportion (40% {49/123}) of hospitals, endoscopes and their accessories appeared to be cleaned inadequately between patients . We conclude that in the majority of hospitals where endoscopies are performed that responded to our survey, there was considerable room for improvement in the cleaning and disinfection of endoscopes. J Antimicrob Chemother, 1989 Sep, 24(3), 355 - 63 Cytotoxicity and uptake of pefloxacin, ciprofloxacin, and ofloxacin in primary cultures of rat hepatocytes; Nordmann P et al.; The cytotoxicity and the uptake of three 4-quinolones--pefloxacin, ciprofloxacin, and ofloxacin--were investigated in primary cultures of rat hepatocytes . As assessed by intracellular enzyme release in culture media, pefloxacin at concentration 400 mg/l and ciprofloxacin at 200 mg/l were found to be hepatotoxins . However, concentration ofloxacin up to 400 mg/l were not hepatotoxic . After 48 h incubation, the remaining antibiotic concentrations in the culture medium as determined by HPLC were 55%, 45%, and 35% for ofloxacin, ciprofloxacin, and pefloxacin, respectively . Comparisons of quinolone concentrations in the hepatocyte culture medium determined by HPLC and correspondent antibacterial activities determined by microbiological assays did not reveal any metabolites with antibacterial activity other than those which have been identified from intact animals. J Antimicrob Chemother, 1989 Sep, 24(3), 317 - 24 In-vitro synergistic activity between ethambutol and fluorinated quinolones against Mycobacterium avium complex; Hoffner SE et al.; Ciprofloxacin, ofloxacin and norfloxacin were ineffective at clinically relevant concentrations against the Mycobacterium avium complex (MAC) in vitro as measured by radiometric respirometry . Only two of 30 clinical isolates of MAC were susceptible to any of the tested quinolones . By contrast good antibacterial activity was obtained when any of the quinolones was combined with ethambutol . The synergistic effect was most pronounced for the combination of ethambutol and ciprofloxacin, to which 76 of 100 strains were susceptible . It is suggested that the synergism is based on an enhanced penetration of the quinolones by ethambutol. Photochem Photobiol, 1989 Sep, 50(3), 287 - 95 Spectroscopic studies of cutaneous photosensitizing agents--XIV . The spin trapping of free radicals formed during the photolysis of halogenated salicylanilide antibacterial agents; Chignell CF et al.; Several antibacterial halogenated salicylanilides, including 3,3',4',5-tetrachlorosalicylanilide (TCSA) and 3,4',5-tribromosalicylanilide (TBSA) are known to cause photoallergy . We have carried out photochemical and spin trapping studies to determine whether free radicals may be involved in the photoallergic response . Irradiation (lambda greater than 300 nm) of TCSA in buffered (pH 7.4) 50% ethanol resulted in the rapid loss of the 3-chloro atom, followed by the much slower release of 5- and then the 4'-chloro atoms to give 3'-chlorosalicylanilide as a stable photoproduct . Under the same conditions TBSA successively lost the 3-, 5- and 4'-bromine atoms to give salicylanilide . When TCSA or TBSA were irradiated (lambda = 356 nm) in buffered (pH 7.4) 50% ethanol containing 2-methyl-2-nitrosopropane (MNP) only solvent-derived free radicals were detected . However, irradiation (lambda = 356 nm) of TCSA and MNP in 0.1 N NaOH generated an ESR spectrum consisting of a broad triplet (aN = 15.6 G) . This spectrum was attributed to the adduct formed by the reaction of MNP with the aryl radical generated by the loss of a chlorine atom from the sterically hindered 3-(or 4'-)-position . Under the same conditions TBSA initially generated a broad triplet (aN = 15.5 G) similar to that observed for TCSA . However, upon further irradiation a 21-line spectrum (aN = 14.4 G, a2H = 2.0 G and a2H = 0.9 G) appeared.(ABSTRACT TRUNCATED AT 250 WORDS) Antibiot Khimioter, 1989 Sep, 34(9), 657 - 62 {A new drug sulfaton in the combined treatment of infections with sulfanilamide derivatives and diaminopyrimidine}; Padeiskaia EN; Derivatives of diaminopyrimidine as potentiators of the effect of the derivatives of sulfanilamide and other antibacterial drugs are discussed . Experimental data on sulfation, a new combined preparation, based on sulfamonomethoxine (a sulfanilamide derivative) and trimethoprim (a diaminopyrimidine derivative) are presented . Brief clinical characteristics of sulfation, its administration routes, doses, dosage advantages and better tolerance as compared to co-trimethoxazole+ (biseptol) are described. Chest, 1989 Sep, 96(3), 528 - 37 Sequential intravenous-oral administration of ciprofloxacin vs ceftazidime in serious bacterial respiratory tract infections; Khan FA et al.; The efficacy and safety of sequential intravenous/oral ciprofloxacin in moderate to severe respiratory tract infections (RTI) were compared with those of ceftazidime in a prospective clinical trial . Sixty-six patients received IV ciprofloxacin (200 to 300 mg twice daily), followed by oral ciprofloxacin (500 mg twice daily) . Fifty-six patients received intravenous ceftazidime (1 to 2 g two to three times daily) . Ciprofloxacin was as effective as ceftazidime and produced a 91 percent clinical cure rate . Significantly more pretreatment bacterial isolates were susceptible to ciprofloxacin, and ciprofloxacin had a significantly higher rate of sputum bacterial eradication than did ceftazidime . Ciprofloxacin showed broad in vitro antibacterial activity with particularly low minimal inhibitory concentrations for Gram-negative organisms . Ciprofloxacin was well tolerated; there were few adverse effects . Ciprofloxacin was an effective and well-tolerated treatment for severe RTI that had the advantages of broad in vitro antibacterial activity, twice-daily dosing, and sequential availability in an intravenous and oral formulation. Antibiot Khimioter, 1989 Sep, 34(9), 696 - 9 {Combined antibacterial therapy of infectious complications in oncological patients}; Smolianskaia AZ; Rational antibacterial therapy of infections in oncological patients in relation to the polyetiological nature of the infections and polyresistance of their causative agents contemplates the use of drug combinations . The necessity of long-term antibacterial therapy in many oncological patients also predisposes to it . The choice of drugs for every patient should stem from bacteriological findings: isolation of the pathogen, its identification and assay of its antibiotic sensitivity . When isolation of the causative agent is not possible or could not be done immediately the drug should be chosen according to the general data on the etiological structure of infectious complications in the particular department and particular pathological process as well as antibiotic sensitivity of the bacteria isolated under such conditions. Antibiot Khimioter, 1989 Sep, 34(9), 662 - 5 {Sensitivity spectrum of Francisella tularensis to antibiotics and synthetic antibacterial drugs}; Vasi'lev NT et al.; Sensitivity of 6 F . tularensis strains to 57 antibiotics and synthetic antibacterial drugs was studied . It was shown that the strains were highly sensitive to aminoglycosides, tetracyclines, anzamycins, quinolones, chloramphenicol, nitrofurantoin, nitroxoline, novobiocin and fusidin and resistant to penicillins, cephalosporins, polypeptides, vancomycin and sulfanylamides . The interrace differences in F . tularensis could be detected only by sensitivity to erythromycin, oleandomycin and spiramycin . There was observed no cross resistance to streptomycin and other aminoglycosides in F . tularensis . Assay of F . tularensis sensitivity to antibacterial drugs of various groups with the rapid photometric procedure and the agar diffusion method revealed that the results were highly comparable. Pharmazie, 1989 Sep, 44(9), 632 - 3 Antibacterial, antifungal and antitumoral activities of 5-carbamoyloxy and 5-acyloxynaphthalene-1,8-carbolactones; Steiman R et al.; Naphthalene-1,8 carbolactone derivatives have been investigated in order to compare their activities using antitumoral, antibacterial and antifungal tests in vitro . The effect of 5-substitution is the reduction of the toxicity and the suppression of the antibiotic activity . The best results were obtained with the ester series (5-acetoxy and 5-propionyloxy) on both antitumoral and antifungal tests. J Anim Sci, 1989 Sep, 67(9), 2341 - 6 Evaluation of a biological response modifier: effects on starter pig performance; Thaler RC et al.; The influence of a biological response modifier (FK-565) on weanling pig performance was evaluated . One hundred twenty-five weanling pigs (weaned at 21 +/- 3 d) averaging 6.3 kg were utilized in a 35-d growth trial . Dietary treatments included a basal diet (1.25% lysine, corn-soybean meal-dried whey), the basal plus .1, 1 or 10 ppm FK-565 and the control plus an antibacterial combination containing chlortetracycline, sulfamethazine and penicillin . Performance was recorded weekly, and on d 35 all pigs were bled for whole blood and serum chemistry profiles and then were euthanatized . Heart, liver, kidneys and spleen weights were recorded . Also, gross and histological examinations were made of these organs, as well as sections of lung, ileum, bone marrow, thymus and mesenteric lymph node . By d 14, pigs fed the antibacterial diet gained faster (P less than .06) than pigs fed the control and FK-565 diets . However, no differences (P less than .10) in feed intake at d 14 or efficiency of feed utilization at either d 14 or 35 were observed . For the overall 35-d trial, ADG was greater (P less than .01) for pigs consuming the antibacterial diet than for pigs consuming control and the FK-565 diets . Pigs consumed more of the antibacterial diet than of the other diets (P less than .05).(ABSTRACT TRUNCATED AT 250 WORDS) Z Orthop Ihre Grenzgeb, 1989 Sep-Oct, 127(5), 587 - 96 {Differentiated surgical and conservative treatment of spondylitis and spondylodiscitis}; Krodel A et al.; In the time from 1980 to 1987 58 patients underwent a conservative or operative treatment of spondylitis and spondylodiscitis according to the individual clinical and radiological features . In early or moderately advanced stages of the disease conservative therapy was performed . Under bedrest and antibacterial or tuberculostatic drug therapy bony fusion of the affected vertebral bodies was achieved in 50% of the pyogenic cases . In tuberculous spondylitis fusion rate was 83% . Persistent septic changes, progressive neurological symptoms and gross vertebral damage are indications for surgery . In those cases removal of the focus and intercorporal spondylodesis was performed . Bony union occurred in every cases . At follow-up examination, 3 years after the onset of therapy on an average, 42 patients had no complaints according to the vertebral column . As the results of our study show spondylitis and spondylodiscitis should according to the clinical and radiological features be lead to a differentiated operative or conservative treatment . Then good clinical results are to be supposed. J Leukoc Biol, 1989 Sep, 46(3), 239 - 45 Lectin-mediated, nonopsonic phagocytosis of type 1 Escherichia coli by human peritoneal macrophages of uremic patients treated by peritoneal dialysis; Boner G et al.; Human peritoneal macrophages isolated from uremic patients undergoing peritoneal dialysis bind type 1 fimbriated Escherichia coli in the absence of opsonins . The number of bacteria bound per macrophage was 6.9, as determined by microscopic examination . Methyl alpha-mannoside (0.1 mM) and p-nitrophenyl alpha-mannoside (0.01 mM) inhibited this binding by about 66% . The ability of peritoneal macrophages to bind E . coli in a mannose-specific manner was confirmed in further experiments using an enzyme-linked immunosorbent assay (ELISA) with an antibacterial antibody, radiolabelled E . coli, and counts of colony-forming units (CFU) . The number of bacteria bound per macrophage was 7 to 12 in the ELISA and 5.5-8.5 in the CFU assay . Methyl alpha-mannoside caused 70% inhibition of binding in the ELISA and 84% in the CFU assay, whereas p-nitrophenyl alpha-mannoside showed inhibition of 79% and 90%, respectively . Most bound bacteria (76-80%) were subsequently killed . Nonfimbriated E . coli 827 bound poorly to the macrophages (approximately 22%) as compared to that of the fimbriated bacteria . Although this binding was not inhibited by methyl alpha-D-mannoside or p-nitrophenyl alpha-mannoside, the percentage of bacteria killed was similar to that of the fimbriated phenotype . The peritoneal macrophage is thus able to phagocytose E . coli in the absence of opsonins . This may explain the relative rarity of E . coli as an etiologic agent of peritoneal infections in the dialysed patient. Am J Dent, 1989 Sep, 2 Spec No, 197 - 206 In vitro and in vivo studies on triclosan/PVM/MA copolymer/NaF combination as an anti-plaque agent; Nabi N et al.; A combination of triclosan, copolymer of PVM/MA and NaF has been optimized in vitro and in vivo for plaque effect . Triclosan (2, 4, 4' trichloro-2'-hydroxydiphenyl ether), a non-cationic antibacterial, was compatible with anionic surfactant, NaF and PVM/MA copolymer as evaluated by in vitro antibacterial tests . The in vitro uptake of triclosan on the saliva-coated hydroxyapatite disks, extracted human teeth and oral buccal epithelial cells was enhanced two fold in the presence of PVM/MA copolymer when compared to the uptake in the absence of the copolymer . The combination consisting of 0.3% triclosan/2% PVM/MA copolymer/1100 ppm NaF was found to be highly effective on reducing smooth and fissure caries, and plaque extent compared to to 1100 ppm/NaF by itself in rats when applied topically . The combination also showed significantly more fluoride uptake and reduction in enamel solubility than 1100 ppm/NaF . The results of these studies indicated that this optimized combination was an effective antiplaque/anticaries agent in vitro and in vivo. Rev Med Chil, 1989 Sep, 117(9), 1037 - 43 {Cephalosporins: bacterial resistance measured by penicillin-binding proteins}; Garrido J et al.; Antibacterial potency of cephalosporins depends on inhibition (acylation) of one or more penicillin-binding proteins (PBP) . Recently, reduced affinity of PBP for cephalosporins and other B-lactam agents has been found in some cases . Mechanism for these changes in affinity are analyzed in this review. West Indian Med J, 1989 Sep, 38(3), 142 - 7 ACTH--inosine pranobex in the treatment of AIDS . Encouraging results; Addo E et al.; Twenty patients with Acquired Immune Deficiency Syndrome (AIDS) received treatment with Inosine Pranobex and specific antibacterial and anti-parasitic therapy . Five died shortly after hospitalization, but a further fifteen who also received ACTH, survived, gained weight and improved clinically, biochemically and haematologically. Philos Trans R Soc Lond B Biol Sci, 1989 Aug 31, 324(1224), 549 - 62 Antibiotics: opportunities for genetic manipulation; Hopwood DA; New antibiotics can still be discovered by the development of novel screening procedures . Notable successes over the last few years include the monobactams, beta-lactamase inhibitors (clavulanic acid) and new glycopeptides in the antibacterial field; antiparasitic agents such as avermectins; and herbicidal antibiotics like bialaphos . In the future we can expect the engineering of genes from 'difficult' pathogens, including mycobacteria and fungi, and cancer cells, to provide increasingly useful in vitro targets for the screening of antibiotics that can kill pathogens and tumours . There will also be a greater awareness of the need to reveal the full potential for antibiotic production on the part of microorganisms by the physiological and/or genetic awakening of 'silent' genes . Nevertheless, the supply of natural antibiotics for direct use or chemical modification is not infinite and there will be increasing scope for widening the range of available antibiotics by genetic engineering . 'Hybrid' antibiotics have been shown to be generated by the transfer of genes on suitable vectors between strains producing chemically related compounds . More exciting is the possibility of generating novelty by the genetic engineering of the synthases that determine the basic structure of antibiotics belonging to such classes as the beta-lactams and polyketides . Research in this area will certainly yield knowledge of considerable scientific interest and probably also of potential applicability . In the improvement of antibiotic titre in actinomycetes, protoplast fusion between divergent selection lines has taken a place alongside random mutation and screening . In some cases the cloning of genes controlling metabolic 'bottlenecks' in fungi and actinomycetes will give an immediate benefit in the conversion of accumulated biosynthetic intermediates to the desired end product . However, the main impact of genetic engineering in titre improvement will probably come only after a further use of this technology to understand and manipulate the regulation of antibiotic biosynthesis as a facet of the general challenge of understanding differential gene expression . Streptomyces offers a particularly fertile field for such research, following the isolation of DNA segments that carry groups of closely linked operons for the biosynthesis of and resistance to particular antibiotics, and of genes with pleiotropic effects on morphological differentiation and secondary metabolite formation. J Chromatogr, 1989 Aug 30, 477(2), 397 - 406 Improvement of chemical analysis of antibiotics . XVI . Simple and rapid determination of residual pyridonecarboxylic acid antibacterials in fish using a prepacked amino cartridge; Ikai Y et al.; A simple and rapid method for the determination of residual pyridonecarboxylic acid antibacterials (PCAs) (oxolinic acid, nalidixic acid and piromidic acid) in fish was developed using a combination of high-performance liquid chromatography (HPLC) and clean-up with an amino-type prepacked cartridge . PCAs were extracted with n-hexane-ethyl acetate (1:3) and the extract was applied to a Baker 10 amino cartridge . PCAs were eluted from the cartridge with acetonitrile-methanol-0.01 M aqueous oxalic acid solution (pH 3.0) (3:1:6) and were determined by HPLC . The separations were performed on Nucleosil 3C18 (3 microns, 75 x 4.6 mm I.D.) using a mobile phase containing oxalic acid . The recoveries of PCAs from various fishes fortified at the level of 1.0 ppm were 77.1-95.5%, and the detection limits were 0.05 ppm . The analytical time per sample was less than 30 min. Pharm Weekbl Sci, 1989 Aug 25, 11(4), 128 - 31 Antibacterial treatment in exacerbations of chronic obstructive pulmonary disease . Pitfalls in study design and evaluation; Wijnands WJ; In studies aimed at assessing the efficacy and safety of antibacterial agents used in treating infections of the respiratory tract, patients with exacerbations of a chronic obstructive pulmonary disease frequently are included . Both the indication for the prescription of an antibiotic and the evaluation of its effect can be difficult . As a general rule, treatment with steroids, bronchodilators and oxygen supply is indicated in cases of exacerbated pulmonary disease . These interventions will influence the clinical and bacteriological parameters usually used to evaluate the antibacterial effect . In a number of cases, non-antibacterial treatment will restore the bronchopulmonary defence sufficiently so that infection control is reached . In order to design meaningful efficacy studies, it is obligatory to understand the pathophysiological mechanisms in chronic obstructive pulmonary disease, to be aware of the pitfalls in making the diagnosis 'bacterial bronchitis' and to take into account the influence of co-medications on the clinical and bacteriological parameters . Some objections to comparative efficacy trials are raised. Nippon Geka Gakkai Zasshi, 1989 Aug, 90(8), 1251 - 7 {Experimental and clinical studies on prevention of vascular prosthetic infection}; Kurata H; Since the treatment of infected vascular prosthetic graft is difficult, it is important to prevent graft infection . At the operation of aneurysmectomy, a part of aneurysmal wall was cultured . As a result, bacterial growth could be seen in 21 out of 58 cases (36%) . In this experiment, expanded polytetrafluoroethylene (E-PTFE) graft was soaked in a solution of tobramycin (TOB) and tested for the prevention of graft infection . First, this E-PTFE graft with a TOB solution was tested for antithrombogenicity and patency rate, and secondly its effect of preventing graft infection was evaluated . 1 . TOB had an effect of antithrombogenicity . 2 . Patency rates of the E-PTFE graft with a TOB solution were as good as those of the graft soaked in a saline solution . 3 . TOB concentration in the grafts was more than 100 micrograms/g after 6 hours from the implantation and more than MIC after 24 hours . 4 . E-PTFE graft with a TOB solution had an effect of antibacteria . This study suggested that E-PTFE graft soaked in a TOB solution was effective to prevent graft infection. J Chemother, 1989 Aug, 1(4), 244 - 7 Antibacterial activity of the dialysates and sera during treatment with chemotherapeutic combinations in continuous ambulatory peritoneal dialysis (CAPD); Beader N et al.; In everyday clinical practice, different chemotherapeutics are mostly applied intraperitoneally in treating continuous ambulatory peritoneal dialysis (CAPD) peritonitis . Antibacterial activity of the dialysates and sera were studied, according to their bacteriostatic effect after the intraperitoneal and/or peroral administration of chemotherapy . All samples were tested by the two-fold dilution method . We found that the best therapeutical effect is obtained by applying the combination of two compatible chemotherapeutics, in which the first acts in the peritoneal cavity, and the other represents the "pool" of chemotherapeutics forming a barrier to the spreading of bacteria into other distant parts of the body. J Chemother, 1989 Aug, 1(4), 223 - 5 Evaluation of ciprofloxacin's activity against recent clinical isolates; Nani E et al.; The in vitro antibacterial activity of ciprofloxacin, a new quinoline carboxylic acid, was tested against 1671 recently clinically isolated bacterial strains, by measuring the minimum inhibitory concentrations (MIC) . Comparisons were made with other quinolones: nalidixic acid, norfloxacin, and other drugs: piperacillin, cefoxitin, cefotetan, ceftazidime, tobramycin, rifampin, tetracycline, chloramphenicol . Ciprofloxacin was very active against the tested species and was the most active drug against all the bacterial strains, with a geometric mean, a MIC50 and MIC90 of 0.27, 0.12 and 2 micrograms/ml, respectively. J Med Chem, 1989 Aug, 32(8), 1749 - 53 N-azamonobactams . 2 . Synthesis of some N-iminoacetic acid and N-glycyl analogues; Curran WV et al.; The synthesis of the title compounds has been accomplished . The N-iminoacetic acid analogues (12a and 12b) containing the aminothiazole type side chain exhibited good in vitro antibacterial activity against Gram-negative organisms . The corresponding N-glycyl derivative (17) was not active. J Periodontol, 1989 Aug, 60(8), 435 - 40 A clinical comparison of antibacterial mouthrinses: effects of chlorhexidine, phenolics, and sanguinarine on dental plaque and gingivitis; Grossman E et al.; This study compared the clinical efficacy of three mouthrinses containing either 0.12% chlorhexidine, phenolic compounds, or sanguinarine, which were used unsupervised, in a placebo-controlled, double-blind study of 6 months' duration . The study was conducted according to ADA clinical guidelines for evaluation of antigingivitis agents and was completed by 481 adults . Following baseline exams and a prophylaxis, subjects were randomly divided into treatment groups matched for age, gender, and gingivitis severity, and were instructed to use the rinses in accordance with manufacturer's directions . Followup examinations evaluated supragingival plaque, gingivitis, and gingival bleeding . Compared to placebo at 6 months, the group rinsing with 0.12% chlorhexidine had significantly less gingivitis (31% reduction), gingival bleeding (39% reduction), and plaque (49% reduction) and was significantly better than any of the other treatment groups (P less than 0.05) . Both the phenolic and sanguinarine groups showed moderate, yet significant, reductions in plaque compared to placebo (24% and 12% respectively) yet were significantly less effective than the 0.12% chlorhexidine rinse (P less than 0.05) . However, neither the phenolic nor sanguinarine rinses were significantly different than placebo in their effects on gingivitis or gingival bleeding . These results support previous published results on the superiority of 0.12% chlorhexidine when used in conjunction with professional care and as an adjunct to routine oral hygiene practices. EMBO J, 1989 Aug, 8(8), 2387 - 91 Apidaecins: antibacterial peptides from honeybees; Casteels P et al.; Although insects lack the basic entities of the vertebrate immune system, such as lymphocytes and immunoglobulins, they have developed alternative defence mechanisms against infections . Different types of peptide factors, exhibiting bactericidal activity, have been detected in some insect species . These humoral factors are induced upon infection . The present report describes the discovery of the apidaecins, isolated from lymph fluid of the honeybee (Apis mellifera) . The apidaecins represent a new family of inducible peptide antibiotics with the following basic structure: GNNRP(V/I)YIPQPRPPHPR(L/I) . These heat-stable, non-helical peptides are active against a wide range of plant-associated bacteria and some human pathogens, through a bacteriostatic rather than a lytic process . Chemically synthesized apidaecins display the same bactericidal activity as their natural counterparts . While only active antibacterial peptides are detectable in adult honeybee lymph, bee larvae contain considerable amounts of inactive precursor molecules. J Med Chem, 1989 Aug, 32(8), 1942 - 9 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents . 12 . 1,2-Dihydroquinolylmethyl analogues with high activity and specificity for bacterial dihydrofolate reductase; Johnson JV et al.; Twelve 2,4-diamino-5-{(1,2-dihydro-6-quinolyl)methyl}pyrimidines containing gem-dimethyl or fluoromethyl substituents at the 2-position of the dihydroquinoline ring were prepared by condensations of dihydroquinolines with 2,4-diamino-5-(hydroxymethyl)pyrimidine . The dihydroquinolines were produced from the reaction of anilines with mesityl oxide or fluoroacetone . In some cases, 1-aryl-2,4-dimethylpyrroles were obtained as byproducts . Most of these pyrimidines were highly inhibitory to Escherichia coli dihydrofolate reductase (DHFR) and also had high specificity for the bacterial enzyme . 2,4-Diamino-5-{{1,2-dihydro-2,4-dimethyl-3-fluoro-2-(fluoromethyl)-8- methoxy-6(1H)quinolyl}methyl}pyrimidine had an apparent Ki value for E . coli DHFR 13 times lower than that of the control, trimethoprim (1), and was 1 order of magnitude more selective for the bacterial enzyme . It had outstanding activity against Gram-positive organisms in vitro, as well as broad-spectrum antibacterial activity equivalent to that of 1 . The results of in vivo testing will be reported elsewhere . The gem-dimethyl substituents of the dihydroquinoline derivatives are considered to be responsible for the high selectivity, as well as contributing to potent bacterial DHFR inhibition . Molecular models are presented which suggest the probable interactions with the bacterial enzyme. J Gen Microbiol, 1989 Aug, 135 ( Pt 8), 2249 - 57 Antibodies to a common outer envelope antigen of Treponema hyodysenteriae with antibacterial activity; Sellwood R et al.; Outer envelopes of Treponema hyodysenteriae strains P18A and VS1 were prepared and characterized by SDS-PAGE . In Western blot analysis of eleven strains of T . hyodysenteriae and two intestinal non-pathogenic spirochaetes, polyclonal antiserum raised to the outer envelopes of strain P18A contained antibodies primarily to two polypeptides . A 45 kDa polypeptide was present in only two strains of T . hyodysenteriae, P18A and MC52/80, whereas another antigen of 16 kDa was common to all eleven strains of T . hyodysenteriae but was not present in the two nonpathogens . Immunogold labelling of whole organisms suggested that the 16 kDa antigen was present on the surface of the spirochaetes . In in vitro tests the serum agglutinated and inhibited growth of only the T . hyodysenteriae strains, suggesting that antibodies to the 16 kDa antigen were responsible for these activities . Serum from a gnotobiotic pig infected with T . hyodysenteriae strain P18A had antibodies to the 16 kDa antigen alone and also possessed agglutinating and growth-inhibitory activities. Vestn Khir Im I I Grek, 1989 Aug, 144(8), 107 - 10 {Errors in the diagnosis and treatment of infection}; Bochorishvili VG et al.; The authors made an analysis of their experience with treatment of sepsis in a specialized center . Typical errors in treatment of the disease in the general public health service are: insufficient sanitation of septic foci, inadequate antibacterial therapy . Not all main possibilities of complex therapy are always used . The problem of struggle against sepsis can not be solved without organization of antiseptic centers. J Antibiot (Tokyo), 1989 Aug, 42(8), 1276 - 82 An unexpected intramolecular cyclization of isothiouronium teicoplanins . II . Reaction mechanism and biological activity; Trani A et al.; N15-Isothiouronium derivatives of teicoplanin and its aglycone submitted to alkaline condition give rise to an intramolecular cyclization . The structures of the new gamma-lactam derivatives were determined by using 1H NMR, IR and fast atom bombardment mass spectra . The cyclization mechanism was interpreted on the basis of the identification of the intermediate structure . The poor in vitro antibacterial activity of the new cyclic compounds and the negligible affinity for the synthetic peptidoglycan model Ac2-L-Lys-D-Ala-D-Ala is probably due to the lack of the N-17 amidic proton and to the lack of the basic character of the nitrogen in position 15. J Antibiot (Tokyo), 1989 Aug, 42(8), 1268 - 75 Thioureas and isothiouronium salts of the aglycone of teicoplanin . I . Synthesis and biological activity; Trani A et al.; A series of thiourea and isothiouronium salt derivatives of the aglycone of teicoplanin was prepared by reaction of the terminal amino group with isothiocyanates, followed by S-alkylation of the thiourea compounds . Unexpectedly, the two classes of derivatives show a similar in vitro antibacterial activity against Gram-positive bacteria . Thiourea compounds, due to the lack of a positively charged N-terminus group, have a 10-fold lower binding constant to Ac-D-Ala-D-Ala, a bacterial cell-wall model, than the parent antibiotic and isothiouronium salt derivatives. J Exp Med, 1989 Aug 1, 170(2), 601 - 6 Prostaglandins from human T suppressor/cytotoxic cells modulate natural killer antibacterial activity; Garcia-Penarrubia P et al.; We have recently described potent antibacterial activity of purified human NK cells . Here we show that this function is regulated by T cytotoxic/suppressor CD8+ cells . Thus, coculture of NK and CD8+ cells for 3 h or longer times abrogated the expression of the NK antibacterial activity, and of two activation markers IL-2R and transferrin receptor (Tf-R) . The suppressive activity was mediated by PGE2 as demonstrated by direct PGE2 determination in CD8+ cell free supernatants, and by inhibition of CD8+ cell suppression with indomethacin or piroxicam in vitro . We also found that resting T cytotoxic/suppressor cells purified by negative selection produce higher amounts of PGE2 than adherent cells like monocytes and macrophages, and that these concentration levels are in the range of concentrations known to suppress a significant number of in vitro immunologic functions. Acta Paediatr Jpn, 1989 Aug, 31(4), 377 - 80 Maternal health, breast-feeding and infant nutrition in Australian aborigines; Gracey M; PIP: Widespread nutritional deficiencies among Australian Aborigine infants are associated with high rates of gastrointestinal and respiratory infections . Also prevalent in this population is a high incidence of low birthweight, which often leads to growth retardation extending throughout the 1st 5 years of life . In a study conducted in Western Australia in 1980, Aboriginal infants were an average of 1.16 kg lighter than their non-Aboriginal counterparts at birth . By 1 year of age, this difference was 2.01 kg for males and 2.23 kg for females; by 5 years of age, the Aborigine differential had reached 3.78 kg for males and 3.15 kg for females . A neglected factor has been the impact of maternal health on this pattern . 1 study of Aborigine women in northwest Australia found that only 40% of women of childbearing age had a satisfactory nutritional status . 25% of these women were overweight . Concentrations of lactoferrin--an iron-binding protein with antibacterial activity--are significantly lower in the breast milk of undernourished mothers . Thus, although traditional Aborigines breastfeed for over 18 months, their milk may be of inadequate quality to confer the protection against infection that is usually a benefit of this form of infant feeding . Thus, an effective approach to reducing the high rates of mortality and morbidity among Aborigine infants would be to target the poor health and nutrition of Aborigine women of reproductive age . J Med Chem, 1989 Aug, 32(8), 1936 - 42 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents . 11 . Quinolylmethyl analogues with basic substituents conveying specificity; Davis SE et al.; A series of nine 2,4-diamino-5-{6-( or 7-)quinolylmethyl}pyrimidines has been prepared by condensations of quinolinecarboxaldehydes with beta-anilinopropionitriles, followed by treatment with guanidine . All compounds has basic or methoxy substituents at the 2- or 4-positions of the quinoline ring . All of the 6-quinolylmethyl derivatives were highly inhibitory against Escherichia coli dihydrofolate reductase (DHFR), provided that an 8-substituent was present in the quinoline ring . Those compounds that had basic substituents in the 2-position of the quinoline ring were also highly specific for bacterial dihydrofolate DHFR, relative to a vertebrate counterpart . Protonation on the quinoline ring nitrogen is a possible cause of specificity. J Med Chem, 1989 Aug, 32(8), 1927 - 35 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents . 10 . 2,4-Diamino-5-(6-quinolylmethyl)- and -{(tetrahydro-6-quinolyl)methyl}pyrimidine derivatives . Further specificity studies; Rauckman BS et al.; A series of 18 2,4-diamino-5-{(1,2,3,4-tetrahydro-6-quinolyl)methyl}pyrimidines has been prepared by the condensation of 2,4-diamino-5-(hydroxymethyl)pyrimidine with 1,2,3,4-tetrahydroquinolines in acidic medium . Several derivatives were catalytically aromatized; others were synthesized from these by routine aromatic substitution or by condensations of (anilinomethyl)pyrimidines to give quinolinylmethyl analogues . Compounds with 4-methyl-8-methoxy substitution are closely related to trimethoprim (1a) in structure and are excellent inhibitors of bacterial dihydrofolate reductase, with activity at least equivalent to that of 1a . The highest degree of inhibition was achieved with the rigid aromatic series, but greater specificity was accomplished among the tetrahydroquinoline derivatives . This was directly related to N-1 substitution of 4-methyl-8-methoxy derivatives . The spatial relationships around N-1 and protonation at this site may both affect selectivity . Such compounds also had excellent broad-spectrum in vitro antibacterial activity. J Med Chem, 1989 Aug, 32(8), 1886 - 90 (3-Amino-2-oxoalkyl)phosphonic acids and their analogues as novel inhibitors of D-alanine:D-alanine ligase; Chakravarty PK et al.; The dipeptide D-alanyl-D-alanine is an essential precursor of bacterial peptidoglycan; thus, blocking its formation is a possible target for the design of novel antibacterial agents . The synthesis of this dipeptide by bacterial D-alanine:D-alanine ligase requires ATP . In analogy with glutamine synthetase, we hypothesized a mechanism for this enzyme involving the intermediacy of D-alanyl phosphate . Several (3-amino-2-oxoalkyl)phosphonic acids and their analogues have been synthesized as possible inhibitory mimics of this proposed intermediate . The most active of them, (3(R)-amino-2-oxobutyl)phosphonic acid (8a) and the corresponding aza analogue (22), were effective ligase inhibitors although they had no significant antibacterial activity . The ligase inhibition of these compounds is consistent with an acyl phosphate displacement step in the mechanism of DAla-DAla ligase. Antibiot Khimioter, 1989 Jul, 34(7), 551 - 5 {Polyantibiotic therapy in the complex treatment of patients with acute diffuse peritonitis}; Bondarev VI et al.; On the basis of the analysis of 217 records of acute diffuse peritonitis peculiarities of the postoperative process of that complication in persons treated with 2 antibiotics (161) and 4 antibacterial drugs (56) were discussed . 4 risk levels were defined with an account of the inflammation process severity . The use of poly-antibiotic therapy was validated . The technique of its application is described in detail . The technique allowed to lower the frequency of postoperative complications and lethality 5-fold. Antibiot Khimioter, 1989 Jul, 34(7), 549 - 51 {Antibacterial therapy in disseminated purulent peritonitis}; Sorokina MI et al.; Analysis of 156 records relating to patients at the age of 15 to 85 years with extended purulent peritonitis of the surgical and gynecological genesis (the toxic phase, VI category ASA) showed that combination of programmed sanitation laparotomy and intensive antibacterial therapy performed as short-term courses before, during and after the operation with an account of the information on the nature of the microbial associations and antibioticograms was an efficient procedure in treatment of severe peritonitis . It was indicated in treatment of patients with polyorgan deficiency . When the surgical treatment was adequate early antibiotic therapy allowed to decrease the number and intensity of postoperative complications: the frequency of abscessing in the abdominal cavity and formation of intestinal fistulas lowered 2 and 1.5 times respectively . Such a decrease was also observed in asthenic patients with lowered protective reactions to development of new infectious foci in the abdominal cavity complicating the peritonitis process . It was also possible to prevent with that procedure the infection generalization and development of peritoneal sepsis . With application of the procedure to such patients (20 per cent) lethality lowered 2-fold. Ortop Travmatol Protez, 1989 Jul, (7), 1 - 4 {Complex prevention of suppurative complications of long surgical procedures using microsurgical technics}; Me'lnikova VM et al.; The authors have demonstrated the efficacy of complex approach to the solution of the problem of postoperative infectious complications in prolonged surgical interventions with application of microsurgical technique in orthopaedic and traumatologic patients . A reduction in the course of prophylaxis with antibiotics in this category of the patients has been substantiated . The use of metabolite therapy in the course of presurgical preparation of the patients under the control of cytochemical investigations allows to carry on the surgery with a more favourable state of the macroorganism . The use of supersonic cavitation for antibacterial treatment of the operative wounds in prolonged interventions with application of microsurgical technique has no specific contraindications . The complex of these measures has allowed to reduce the rate of suppurations after prolonged surgical interventions with application of microsurgical technique from 23.01 to 8%. J Pharm Sci, 1989 Jul, 78(7), 585 - 8 Synthesis and in vitro antibacterial activity of some 1-(difluoromethoxyphenyl)quinolone-3-carboxylic acids; Xiao W et al.; We report on the synthesis of N-1-phenylquinolones in which the difluoromethoxy moiety is utilized as a halogen replacement . The antibacterial activity is discussed with reference to N-1-halophenylquinolones. Jpn J Pharmacol, 1989 Jul, 50(3), 283 - 8 Studies on oxacephem antibiotics: comparison of the effects of 1-oxa and 1-thia cephalosporins on blood coagulation activities and vitamin K metabolism in rats; Uchida K et al.; Oxacephem antibiotics have been developed to increase the antibacterial activity of cephem antibiotics, but the effect of 1-oxygen replacement of cephem antibiotics on blood coagulation activities is not yet known . Therefore, latamoxef (LMOX), flomoxef (FMOX) and their 1-S congeners were examined for their effects on prothrombin time, activated partial thromboplastin time, plasma prothrombin and Factor VII levels, plasma and liver descarboxyprothrombin (PIVKA-II) levels, and liver microsomal vitamin K epoxide reductase activities in rats kept on a vitamin K-deficient diet . Under the vitamin-deficient states, LMOX, FMOX and their 1-S congeners inhibited the vitamin K epoxide reductase, although the effect of FMOX or its congener was much less than that of LMOX, and they decreased the blood clotting activities in rats fed a vitamin K-deficient diet . However, no difference was found in these effects between LMOX and its 1-S congener or between FMOX and its 1-S congener . This result suggests that the 1-oxygen replacement of cephem antibiotics is not responsible for the hypoprothrombinemic effect of the antibiotics. J Antibiot (Tokyo), 1989 Jul, 42(7), 1114 - 23 Chemical modification of hitachimycin . III . Synthesis and antitumor activities of amino acyl derivatives; Shibata K et al.; Amino acyl derivatives of hitachimycin have been synthesized and evaluated their activities including antibacterial, cytocidal against HeLa cells and in vivo antitumor against sarcoma 180 . 15-O-(tert-Butoxycarbonyl(BOC)-glycyl)hitachimycin (2), 15-O-(BOC-beta-alanyl)hitachimycin (4), 15-O-(BOC-(O-tert-Bu)-glutamyl)hitachimycin (6) and 15-O-L-alanylhitachimycin (11) showed comparable in vivo antitumor activity with hitachimycin and the solubility of these compounds was improved. J Antibiot (Tokyo), 1989 Jul, 42(7), 1100 - 13 Synthesis and antibacterial activity of 5-methylcarbapenems; Onoue H et al.; Four possible racemic isomers of N-acetyl-5-methylthienamycin derivatives were synthesized and their antibacterial activities are discussed in relation to their physico-chemical properties . 5-Methylcarbapenems having various C-2 side chains were also prepared. J Antibiot (Tokyo), 1989 Jul, 42(7), 1037 - 42 Studies on a novel antitumor antibiotic, phenazinomycin: taxonomy, fermentation, isolation, and physicochemical and biological characteristics; Omura S et al.; A new antibiotic, phenazinomycin (C27H32N2O, MW 400), was isolated from the cultural mycelium of Streptomyces sp . WK-2057 . This antibiotic possesses antibacterial activities against Gram-positive bacteria in vitro, direct cytotoxic activities against HeLa S3, P388 and P388 doxorubicin-resistant cells in vitro and antitumor activities against experimental murine tumors in vivo. Antibiot Khimioter, 1989 Jul, 34(7), 545 - 8 {Antibacterial prophylaxis and treatment of wound infection in the light of the development of the ideas of Z . V . Ermol'eva}; Mel'nikova VM et al.; At present we use antibiotics in treatment of wound infections on the basis of the teaching of Z . V . Ermolyeva on their prophylactic and therapeutic value developed during the Great Patriotic War . We consider that along with thorough primary surgical treatment the use of antibiotics in cases with open fracture is indicated . In "clear" operations on the bones and joints we use antibiotics only in patients with risk of infection . In cases with purulent infection and isolation of multicomponent microbial associations from the wound including also nonsporulating anaerobic organisms we mostly apply combined antibacterial chemotherapy with immunotherapy and surgical treatment. Stomatologiia (Mosk), 1989 Jul-Aug, 68(4), 15 - 8 {The use of lysoamidase for treating complications of caries and diseases of the periodontium and oral mucosa}; Borovskii EV et al.; Antibacterial and proteolytic enzyme lysoamidase was used to treat periodontitis and a range of diseases of oral mucosa . The results displayed its major advantages over trypsin and allowed us to recommend it as an effective means of local treatment in the combined therapy of these disorders. Rev Infect Dis, 1989 Jul-Aug, 11 Suppl 5, S979 - 84 Use of fluoroquinolones for intracellular pathogens; Pocidalo JJ; Current microbiologic techniques (determinations of minimal inhibitory and/or microbicidal concentrations) are unable to delineate the true role of anti-infectious drugs in the treatment of human infections due to intracellular pathogens . The prediction and evaluation of the efficacy of quinolones against intracellular pathogens requires information on four different steps . (1) Quinolones should be able to penetrate phagocytes; intramacrophagic concentration is highly dependent on serum pharmacokinetics; finally, the best quinolone should have the longest serum half-life and reach highest maximum serum concentrations . (2) The evaluation of antibacterial activity requires an adequate cellular model (e.g., multiplication of Legionella pneumophila within human monocyte-derived macrophages) . (3) The prediction of drug efficacy requires an experimental animal model . (4) Clinical trials in human disease are necessary . This stage is difficult when the evaluation concerns severe infectious diseases because the rarity of these diseases makes random clinical trials difficult . In this paper we describe methodologies for assessing the efficacy of quinolones against intracellular bacterial pathogens with a particular focus on Legionella pneumophila. J Med Microbiol, 1989 Jul, 29(3), 221 - 7 Interactions of the 4-quinolones with other antibacterials; Lewin CS et al.; The effect of sub-inhibitory concentrations of 16 antibacterials on the bactericidal activity of the 4-quinolones nalidixic acid, ciprofloxacin and ofloxacin against Escherichia coli KL16 in nutrient broth was investigated . Sub-inhibitory concentrations of rifampicin, clindamycin, chloramphenicol, erythromycin or tetracycline antagonised the bactericidal activity of the 4-quinolones . Conversely, all seven aminoglycosides tested enhanced the bactericidal activity of the 4-quinolones whereas the cell wall antagonists, azlocillin, mezlocillin, ceftazidime and vancomycin had no effect on the bactericidal activity of the 4-quinolones. Acta Haematol Pol, 1989 Jul-Dec, 20(2), 201 - 5 {Phagocytic activity of platelets in patients with pneumonia}; Kemona H et al.; In 22 patients with pneumonia the per cent of phagocytizing platelets and the phagocytosis index of the platelets were determined before treatment and in 14 patients this was done after treatment . Before treatment the per cent of phagocytizing platelets was 1.37%, on average, and after treatment it was 1.20, and it was thus much lower than in the control group X 2.33 . The phagocytosis index before treatment was 1.39 on average, and after treatment it was 1.28, while in the control group it was 1.54 . The obtained results seem to indicate that in pneumonia platelets participate in the antibacterial processes and the lungs as a thrombopoietic organ contribute to this phenomenon. Farmaco, 1989 Jul-Aug, 44(7-8), 695 - 702 Individual degradation rate constants for cefotaxime, deacetylation profile; Fabre H et al.; The individual degradation rate constants for cefotaxime in aqueous solution were calculated within a pH range of 1.6-10.0 at 37 degrees C from high performance liquid chromatography data . This allowed the general degradation profile of cefotaxime to be decomposed into a degradation profile attributed to the opening of the beta-lactam nucleus and a degradation profile attributed to the deacetylation . From the calculations of the individual rate constants, the activity of degraded cefotaxime solutions could be predicted . In the pH range of injectable solutions of cefotaxime 5-7, roughly equivalent amounts of inactive beta-lactam cleavage products and deacetylated compound which has a different spectrum of antibacterial activity are formed. Rev Infect Dis, 1989 Jul-Aug, 11 Suppl 5, S941 - 6 Quinolone uptake by bacteria and bacterial killing; Diver JM; A review of the mechanisms of the action of 4-quinolones is presented, concentrating on the process of uptake and bacterial killing . 4-Quinolones appear to cross the gram-negative outer membrane via diffusion through outer-membrane proteins, although disruption of the normal outer-membrane barrier by 4-quinolones may facilitate diffusion via a non-porin-mediated route . Accumulation in the cytoplasm may involve influx and efflux mechanisms . The inhibition of DNA synthesis by 4-quinolones has been investigated in Escherichia coli AB1157 and found to correlate with antibacterial activity (as measured by the minimal inhibitory concentration) . 4-Quinolones have other pleotropic effects on bacterial cells, such as induction of the SOS (DNA repair) response, filamentation, and direct effects on membranes. Infect Immun, 1989 Jul, 57(7), 2196 - 202 Relationship between neutrophil-mediated oxidative injury during acute experimental pyelonephritis and chronic renal scarring; Meylan PR et al.; Previous experiments with rats have suggested that pyelonephritic scarring after acute ascending Escherichia coli pyelonephritis partly results from excessive polymorphonuclear leukocyte (PMN) infiltration and activation in the kidney parenchyma . We have studied the role of PMN oxidative metabolism in generating tissue injury during acute pyelonephritis . Rats with acute pyelonephritis were treated with dapsone (25 mg/kg twice daily for 3 days), a compound known to prevent PMN oxidant damage . In vitro, levels of dapsone easily achieved in vivo inhibited myeloperoxidase (MPO)-mediated reactions involving the oxidation of halides to reactive cytotoxic hypohalites (such as MPO-mediated iodination and luminol-enhanced chemiluminescence) . In contrast, dapsone had no effect on superoxide production, lysosomal enzyme release, or bacterial killing by activated PMN . In vivo, dapsone treatment had no significant effect on acute pyelonephritis with respect to (i) bacterial counts, (ii) inflammatory swelling, and (iii) PMN infiltration . However, dapsone-treated animals sacrificed 2 months after acute pyelonephritis had a 65% reduction of renal scars when compared with controls . Since dapsone had no antibacterial effect, this protection is compatible with the hypothesis that dapsone prevented oxidant-generated tissue injury due to the extracellular release of the MPO system by activated PMN during acute suppurative pyelonephritis. J Antibiot (Tokyo), 1989 Jul, 42(7), 1124 - 32 Synthesis and biological activity of 7 alpha-hydroxyethyl-1-oxacephem derivatives; Nishimura S et al.; A series of 7 alpha-hydroxyethyl-1-oxacephems (1) was synthesized . The main focus of this study was to investigate biological activity relationships between 1-oxacephems (1) and the corresponding cephems (2) . Replacement of the sulfur atom of 2 by the oxygen atom caused an enhancement of antibacterial activity, although the antibacterial activity of 1 was not high enough . Additionally 1 showed beta-lactamase inhibitory activity, especially against cephalosporinase . However, the potency was lower than that of 2. J Biol Chem, 1989 Jun 15, 264(17), 9768 - 71 Canavanine incorporation into the antibacterial proteins of the fly, Phormia terranovae (Diptera), and its effect on biological activity; Rosenthal GA et al.; In response to microbial infection or mechanical injury, larvae of the fly, Phormia terranovae (Diptera), can induce de novo production of a group of antibacterial proteins including: peak I protein, diptericin A, diptericin B, diptericin C, and peak V protein . Administration of L-canavanine at the time of mechanical injury results in the incorporation of this arginine antagonist into these proteins . Canavanine replacement for arginine causes a total loss of detectable antibacterial activity for diptericin B and diptericin C, whereas diptericin A and peak V protein are severely inhibited . This loss in biological activity occurs in spite of the fact that canavanine stimulates induced protein synthesis . Analysis of the hydrolysate of diptericin A reveals that one-third of the 3 arginyl residues are replaced by canavanine . This investigation provides the first evidence that canavanine incorporation into a protein can impair its function. Eur J Biochem, 1989 Jun 15, 182(2), 423 - 7 Insect immunity . Isolation of cDNA clones corresponding to diptericin, an inducible antibacterial peptide from Phormia terranovae (Diptera) . Transcriptional profiles during immunization; Reichhart JM et al.; We have previously isolated and characterized a family of novel 8-kDa cationic antibacterial peptides synthesized by larvae of Phormia terranovae (Diptera) in response to various injuries . These molecules have been named diptericins . The peptide sequence of diptericin A was used to prepare oligonucleotides for screening cDNA libraries and we report in the present paper the isolation of several cDNA clones encoding diptericin . The analysis of the nucleotide sequences indicates that diptericin is synthesized as a prepeptide which is matured in two steps: (a) cleavage of a signal peptide and (b) amidation of the C-terminal residue . Interestingly, the 3' untranslated region of the mRNA contains a consensus sequence TTATTTAT which is also observed in the mRNA of another insect antibacterial peptide (attacin-related sarcotoxin IIA) and in mRNAs encoding proteins related to the inflammatory response in mammals . Our data illustrate that diptericins form a polymorphic family of immune peptides . The transcription of the diptericin genes is rapidly induced in the fat body after inoculation of bacteria, as evidenced by the transcriptional profile. Yakugaku Zasshi, 1989 Jun, 109(6), 377 - 87 {Synthetic cephalosporins . III . Synthesis and antibacterial activity of 7-{2-(2-Aminothiazol-4-yl)-3-carboxy-2-propenoamido}cep hal osporins and related compounds}; Sakagami K et al.; Synthesis and antibacterial activity of 7-{2-(2-aminothiazol-4-yl)-3-carboxy-2-propenoamido}cepha los porins and their derivatives are described . These compounds are of interest as carbon analogues of oximecephalosporins, 7-{2-(2-aminothiazol-4-yl)-2(Z)-oxyiminoacetamido}cephalo spo rins having remarkable antibacterial activity . The synthesized 7-{2-(2-aminothiazol-4-yl)-3(Z)-carboxy-2-propenoamido}-c eph alosporins (14, 19) show improved activity especially against the beta-lactamase-producing strains . A 7-{2-(2-aminothiazol-4-yl) maleimido}cephalosporin (15) has been also prepared by cyclization of 7-{3-(2-aminothiazol-4-yl)-2-ethoxycarbonyl-2(Z)-propenoamido++ +}cephalosporin. Antibiot Khimioter, 1989 Jun, 34(6), 420 - 5 {Micro-ecological aspects of studies on the effect of antibacterial drugs on intestinal microflora}; Mikel'saar ME et al.; Possible characterization of intestinal microflora as an integral system after exposure to antibacterial drugs was studied . Microflora of the contents and mucosa of the jejunum and large intestine in control rats and in rats exposed to metronidazole was studied and numerical indicators characterizing ratios of dominating and accompanying microbial groups in the intestine biotope++ were developed . With this purpose the proportion of the microbial groups in the total quantity of the microbes of a microbiocenosis was determined by the data on microflora quantitative composition . On the basis of detected wide species variety of microorganisms potentially dominating by their biotope numerical limits of the norm were determined only for the microbial groups of the accompanying microflora . The total proportion of the accompanying microbial populations under the normal conditions and the detected measure of deviation (reverse, partial) from the ratio of the dominating and accompanying microorganisms peculiar of the given biotope++ in separate subjects promoted estimation of microbiocenoses of definite biotope of the intestine as a whole. Pathol Biol (Paris), 1989 Jun, 37(5 Pt 2), 517 - 22 {In vitro bactericidal effect of a piperacillin-pefloxacin combination against isolated strains of nosocomial pneumopathies in intensive care}; Simeon De Buochberg M et al.; Combinations of piperacillin and pefloxacin are evaluated in vitro using checkerboard and killing-curves methods against 19 clinical isolates: S . aureus, K . pneumoniae, K . oxytoca, C . freundii, P . stuartii, Ps . aeruginosa, Ps . maltophilia and Ac . anitratum . The static checkerboard method showed more synergistic antibacterial effects than the killing curves method . The best synergistic effects appeared against S . aureus, K . oxytoca, P . stuartii, Ps . aeruginosa Ac . anitratum, including a notable increase of the rapidity of bactericidal activity . The combination PIP 64 micrograms - PEF 4 micrograms prevents the frequent secondary regrowth seen after 6 hours with the antibiotics used alone . No activity is obtained against S . aureus meti-R and Ps . maltophilia. Jpn J Antibiot, 1989 Jun, 42(6), 1346 - 57 {Laboratory and clinical investigations of cefodizime in infectious diseases in childhood}; Komada Y et al.; In this study, cefodizime (CDZM, THR-221) was administered to 34 children with infections and the efficacy was evaluated in 30 patients . The efficacy rate was 90.0% and CDZM was proved to be a highly effective antibiotic for infectious diseases in childhood . We also demonstrated that CDZM had strong antibacterial activities against both Gram-positive and Gram-negative bacteria . No severe toxicity related to intravenous injection of CDZM was observed in our 34 cases. J Comput Aided Mol Des, 1989 Jun, 3(2), 149 - 64 Highly conformationally constrained halogenated 6-spiroepoxypenicillins as probes for the bioactive side-chain conformation of benzylpenicillin; Shute RE et al.; The halogenated 6-spiroepoxypenicillins are a series of novel semisynthetic beta-lactam compounds with highly conformationally restricted side chains incorporating an epoxide . Their biological activity profiles depend crucially on the configuration at position C-3 of that epoxide . In derivatives with aromatic-containing side chains, e.g., anilide, the 3R-compounds possess notable Gram-positive antibacterial activity and potent beta-lactamase inhibitory properties . The comparable 3S-compounds are antibacterially inactive, but retain beta-lactamase inhibitory activity . Using the molecular simulation programs COSMIC and ASTRAL, we attempted to map a putative, lipophilic accessory binding site on the PBPs that must interact with the side-chain aromatic residue . Comparative computer-assisted modelling of the 3R-, and 3S-anilides, along with benzylpenicillin, indicated that the available conformational space at room temperature for the side chains of the 3R- and the 3S-anilides was mutually exclusive . The conformational space for the more flexible benzylpenicillin could accommodate the side chains of both the constrained penicillin derivatives . By a combination of van der Waals surface calculations and a pharmacophoric distance approach, closely coincident conformers of the 3R-anilide and benzylpenicillin were identified . These conformers must be related to the antibacterial, 'bioactive' conformer for the classical beta-lactam antibiotics . From these proposed bioactive conformations, a model for the binding of benzylpenicillin to the PBPs relating the three-dimensional arrangement of a putative lipophilic S2-subsite, specific for the side-chain aromatic moiety, and the 3 alpha-carboxylate functionality is presented. Int J Pept Protein Res, 1989 Jun, 33(6), 412 - 21 Design, synthesis and antibacterial activity of cecropin-like model peptides; Fink J et al.; In order to investigate structure-activity relationships of cecropins, model peptides that mimic certain structural features of the cecropin molecules were designed and synthesized . The conformational analysis of cecropins and the design of the model peptides were based on Chou-Fasman calculations . The peptides were synthesized by solid-phase methods and purified by reverse-phase liquid-chromatography on C18-silica columns . Their secondary structures were studied by circular dichroism measurements . Antibacterial activities against seven test organisms were determined and compared to the activities of the natural cecropins A and B . These results were discussed on the basis of structural features of the model peptides and on model mechanisms . It was concluded that high antibacterial activity for this class of compounds requires a basic helical amphipathic N-terminal segment that is connected to a hydrophobic helical C-terminal segment by a flexible non-helical hinge region. Pharm Res, 1989 Jun, 6(6), 486 - 91 Prediction of the distribution volumes of cefazolin and tobramycin in obese children based on physiological pharmacokinetic concepts; Koshida R et al.; So as to estimate the appropriate dose of antibacterial drugs in obese children, prediction of the volume of distribution in these children was attempted based on physiological pharmacokinetic concepts which had been constructed from results in normal-weight