J Clin Pharmacol, 1978 Oct, 18(10), 491 - 9 Cinoxacin: pharmacokinetics and the effect of probenecid; Israel KS et al.; Cinoxacin is a new synthetic organic antibacterial compound which has a serum half-life of approximately 1 hour . Most of the drug is eliminated in man by the kidney, primarily as unchanged drug . The renal clearance of cinoxacin is slightly greater than the usually accepted value for the average glomerular filtration rate, which suggests that it is probably filtered and is also secreted by the tubule . Results after pretreatment with probenecid further suggest secretion of the drug. J Antibiot (Tokyo), 1978 Oct, 31(10), 945 - 8 The isolation and characterization of rubradirin B; Hoeksema H et al.; Rubradirin B, C40H33N3O15, was separated from other components of the rubradirin complex by chromatographic and crystallization procedures . The spectrum of antibacterial activity is similar to that of rubradirin, but the antibiotic is less active. Appl Environ Microbiol, 1978 Oct, 36(4), 577 - 83 Isolation, purification, and antibiotic activity of o-methoxycinnamaldehyde from cinnamon; Morozumi S; o-Methoxycinnamaldehyde has been isolated and purified from powdered cinnamon . The compound inhibits the growth and toxin production of mycotoxin-producing fungi . The substance completely inhibited the growth of Aspergillus parasiticus and A . flavus at 100 microgram/ml and A . ochraceus and A . versicolor at 200 microgram/ml . It inhibited the production of aflatoxin B1 by over 90% at 6.25 microgram/ml, ochratoxin A at 25 microgram/ml, and sterigmatocystin at 50 microgram/ml . The substance also displayed a strong inhibitory effect on the growth of five dermatophytoses species, e.g., Microsporum canis (minimum inhibitory concentration, 3.12 to 6.25 microgram/ml) . However, no antibacterial effect was observed at concentrations as high as 50 microgram/ml. J Bone Joint Surg Am, 1978 Oct, 60(7), 871 - 81 Treatment of orthopaedic infections with electrically generated silver ions . A preliminary report; Becker RO et al.; Electrically generated silver ions have been shown previously to be a potent antibacterial agent with an exceptionally broad spectrum as indicated by in vitro testing . The present study reports on clinical experience using electrically generated silver ions as adjunctive treatment in the management of chronic osteomyelitis . Fourteen patients had fifteen treatment attempts: thirteen for chronic osteomyelitis of the tibia, one for acute and chronic pyarthrosis and osteomyelitis of the knee, and one for a chronically draining sinus after total hip replacement . Wound debridement, silver ion iontophoresis, and subsequent wound care (usually provided by the patient) resulted in control of the infection in twelve of the fifteen treatment attempts and in healing of the non-union after follow-up ranging from three to thirty-six months . The other three attempts led to two partial and one complete failure. Ric Clin Lab, 1978 Oct-Dec, 8(4), 211 - 31 Human lysozyme (origin and distribution in health and disease); Reitamo S et al.; Histochemical and in particular immunoperoxidase techniques have extended our knowledge about the cellular distribution of LZM . The enzyme has been detected in: 1 . granulocytes, which synthesize LZM in bone marrow; 2 . cells of the mononuclear phagocytic system, which synthesize LZM continuously; 3 . various exocrine glands, whose LZM is probably in part synthesized locally and in part derived from blood; 4 . cartilage, which probably synthesizes LZM and 5 . the kidney, in which LZM is serum-derived . In pathological conditions, such as inflammation and neoplasia, most LZM-positive cells at the site of disease are either granulocytes or members of the mono-nuclear phagocytic system . A notable exception are the metaplastic Paneth cells that occur along the gastrointestinal tract in inflammation and neoplasia . LZM is an antibacterial agent, but evidence is accumulating which suggests that the enzyme might have other functions as well. Urology, 1978 Oct, 12(4), 411 - 5 Heparin as antibacterial agent in rabbit bladder; Hanno PM et al.; Previous studies performed in our laboratory indicated that the primary antibacterial defense mechanism of the rabbit bladder is the antiadsorptive action of the surface mucopolysaccharide . The increased bacterial adsorption that occurs when the bladder is denuded of this layer was prevented by the instillation of heparin . Additional studies showed that the protective effect of heparin is inhibited by protamine, a further indication that the bladder's "antiadherence factor" is a mucopolysaccharide . Small amounts of heparin, applied directly to the mucoprotein-deficient bladder or to the surface of the inoculated bacteria, produced a statistically significant reduction in bacterial adsorption. Immun Infekt, 1978 Oct, 6(5), 180 - 93 {The present situation of antibacterial resistance (author's transl)}; Wagner WH; The various types of bacterial resistance (natural species resistance, chromosomal and plasmidic resistance) and their mechanisms are described . Thereafter, a survey on the resistance is given using investigations from different sources . The distribution of resistant strains dependent on the geographical location and the situation of the patients (ambulatory--hospitalized) is described, and the development of resistant strains in dependance of time is analyzed . Finally, the phenomena of resistance against aminoglycoside and beta-lactam antibiotics are explained in more detail. J Antibiot (Tokyo), 1978 Oct, 31(10), 991 - 6 1- and 3-deamidino derivatives of dihydrostreptomycin and some 1-N-acyl derivatives; Usui T et al.; 1-Deamidino-, 3-deamidino- and 1,3-di(deamidino)dihydrostreptomycin (1, 2, 3) were prepared by treatment of dihydrostreptomycin (DHSM) with ammonia at 100 degrees C . The 3-guanidino group of DHSM is suggested to be more important than the 1-guanidino group for the antibacterial activity of DHSM . 1-N-{(S)-4-Amino-2-hydroxybutyryl) and 1-N-{(S)-4-guanidino-2-hydroxybutyryl} derivatives (4, 6) of 1-deamidinodihydrostreptomycin were futher prepared. Chem Biol Interact, 1978 Sep, 22(2-3), 167 - 83 Effects of halogenated antibacterials on the erythrocyte membrane; Miller TL et al.; The influence of halogenated antibacterials on membrane structure and function was investigated using the human erythrocyte membrane as a model . Measurements of hemolysis in isotonic solution, altered membrane permeability, and stabilization against hypotonic hemolysis resulting from exposure of erythrocytes to halogenated antibacterials served as criteria of membrane-related effects . The hemolytic potency of the compounds studied differed widely, decreasing in the order hexachlorophene (HCP) greater than 2,2'-methylenebis(3,5-dichlorophenol) (3,5-TCP) greater than 2,2'-methylenebis(3,4-dichlorophenol) (3,4-TCP) approximately equal to 2,2'-methylenebis(4,6-dichlorophenol) (4,6-TCP) greater than 2,2'-methylenebis(4-chlorophenol) (DCP) greater than 3,4'-tribromosalicylanilide (TBS) approximately equal to 3,3',4',5-tetrachlorosalicylanilide (TCSA) . Each of the antibacterials tested stabilized the erythrocyte against hypotonic hemolysis, although there were marked differences in the concentrations required to afford maximum stabilization as well as in the extent of protection . The observed order of protective effectiveness was HCP greater than 3,4-TCP greater than 4,6-TCP greater than DCP approximately equal to TCS greater than TBS . As shown by measurements of the first-order rate constant for K+ efflux, the permeability of the erythrocyte membrane to K+ was increased upon exposure to the antibacterials, with the effect of HCP greater than 3,4-TCP greater than 4,6-TCP approximately equal to 3,4-TCP greater than DCP approximately equal to TCS greater than TBS . These results indicate that halogenated antibacterials are capable of perturbing mammalian membranes, a feature which may account in part for their mammalian toxicity. Tijdschr Diergeneeskd, 1978 Sep 1, 103(17), 899 - 906 {Nalidixic acid intoxication in two pregnant bitches (author's transl)}; Solleveld HA et al.; To ensure prolonged survival, dogs with cyclic neutropenia should be protected against bacterial infection of exogenous or endogenous origin, particularly during the neutropenic episodes . One of the methods available to minimize the risk of infection in these dogs, is selective decontamination of the gastrointestinal tract by using antibiotics and/or chemotherapeutic agents, in conjunction with housing in a laminar-flow cabinet . Two pregnant bitches, some of the offspring of which were expected to be homozygous for the cyclic neutropenia allele, were decontaminated with nalidixic acid . Fourteen days after initiation of the antibacterial treatment, the two dogs died . Jaundice and seizures had been apparent in both animals prior to death . Histopathological examination revealed changes primarily in the liver, which were consistent with toxic hepatic necrosis and were characterized by severe centrilobular haemorrhage and disappearance of hepatocytes . Multiple haemorrhages were observed in other organs . Further clinical investigation in two other dogs strongly suggested that nalidixic acid was the cause of death in the two pregnant bitches. J Pharm Sci, 1978 Sep, 67(9), 1336 - 8 Selenium heterocycles XXII: Synthesis and antibacterial antifungal activities of arylsulfonyl-1,2,3-selenadiazoles; Lalezari I et al.; Series of 4-arylsulfonylmethyl-1,2,3-selenadiazoles, 4-(1-arylsulfonylethyl)-1,2,3-selenadiazoles, and 4-alkyl (or aryl)-5-arylsulfonyl-1,2,3-selenadiazoles were synthesized . 4-(3-Pyridyl)-5-phenylsulfonyl-1,2,3-selenadiazole exhibited the highest activity of growth inhibition against some bacteria and fungi. Rev Cubana Med Trop, 1978 Sep-Dec, 30(3), 167 - 73 {Preparation and evaluation of antibacterial activity of partial fractions of Vallesia antillana Wood}; Rojas Hernandez NM et al.; A study on the antibacterial properties of alkaloidal fractions of Vallesia antillana Wood, a Cuban plant belonging to the Apocynaceae family, is performed for the first time . Four partial fractions from bark of stems were prepared according to a classical extraction of total alkaloids and a partial fractionation of these, with the use of tartaric acid and ethyl ether and by a pH gradient with values of 2.5, 5.0, 7.0 and alkaline one . Data from thin layer chromatography on the alkaloidal content of different fractions are added and an assessment of antibacterial activity was made; for this, a method of sections in agar medium with bacterial species of human clinical interest was used; inhibitory halos found within 24 hours of incubation at 37 degrees C are reported in millimeters. J Dent Res, 1978 Sep-Oct, 57(9-10), 922 - 6 Inhibition and killing of oral bacteria by silver ions generated with low intensity direct current; Thibodeau EA et al.; Silver cations generated by passing low intensity direct current through pure silver electrodes were found to be sufficiently antibacterial to cause sterilization of samples of infected dentin . The optimal procedure involved a 5 microA current applied for 20 minutes with the anode then left in contact with the sample . Minimal inhibitory concentrations of electrically generated silver ions for representative oral bacteria were essentially equal to those for silver ions added as nitrate or fluoride salts, and medium constituents, including sodium thioglycolate, antagonized antibacterial action . A major advantage to the use of the electrode method is that it allows for continuous, focal application of antibacterial silver cations. J Antibiot (Tokyo), 1978 Sep, 31(9), 906 - 10 Effects of polymyxin antibiotics on iodohippurate accumulation in rabbit renal cortical slices; Milman N et al.; The in vitro effects of polymyxin antibiotics on 0-125I-hippurate (OIH) accumulation in rabbit renal cortical slices were studied using incubation media with pH ranging from 6.9 to 7.9 and containing polymyxin B sulfate, colistin sulfate, sodium colistimethate and antibacterially inactive N-succinyl colistin in concentrations ranging from 1 to 2,000 microgram base/ml . Polymyxin B, colistin and colistimethate depressed OIH accumulation significantly in concentrations greater than or equal to 300 microgram/ml . The effects on accumulation were clearly pH-dependent and most pronounced at alkaline pH . N-Succinyl colistin had only a marginal influence on accumulation, even in high concentrations . Colistimethate produced a significantly smaller decrease in accumulation at all pH values than both polymyxin B and colistin . The results suggest that the presence of free amino groups is necessary to obtain a decrease in accumulation and correlate with the known in vivo nephrotoxicity of these antibiotics. Am J Physiol, 1978 Sep, 235(3), C103 - 8 Reactive forms of oxygen and chemiluminescence in phagocytizing rabbit alveolar macrophages; Miles PR et al.; Chemiluminescence (CL), superoxide anion (O2-) production, and particle uptake were measured to determine the role of antibacterial substances in the chemiluminescent response associated with phagocytosis in rabbit alveolar macrophages (AM) . Exposure of AM to zymosan particles induced both CL and the production of extracellular O2- . CL is inhibited by superoxide dismutase, an enzyme which catalyzes the conversion of O2- to hydrogen peroxide (H2O2), by catalase, an enzyme which destroys H2O2, and by the hydroxyl radical (.OH) scavengers, benzoate and ethanol . Superoxide dismutase and catalase probably exert their effects in the extracellular fluid . CL can also be produced by the addition of NaO2 or H2O2 to zymosan in a noncellular system . The chemiluminescent response occurs before particle uptake is complete, which also indicates that CL occurs in the extracellular fluid . These results suggest that CL induced by zymosan in AM is due to the extracellular reaction between various reactive forms of oxygen and zymosan. Gastroenterology, 1978 Sep, 75(3), 445 - 9 Endotoxin and the liver . III . Modification of acute carbon tetrachloride injury by polymyxin b--an antiendotoxin; Nolan JP et al.; Previous work suggests that endotoxin of enteric origin may contribute to both acute and chronic liver injury by other agents . In particular, evidence exists that endotoxin tolerance modifies biochemical and histological evidence of carbon tetrachloride hepatotoxicity . The present study was undertaken to ascertain whether another method of modifying endotoxicity would protect against carbon tetrachloride (CCl4) damage as well . The antibiotic polymyxin B (PB) has unique antiendotoxin properties not shared by gentamicin sulfate, an antibiotic with a similar antibacterial spectrum . In groups of rats pretreated with either PB, gentamicin, or diluent, the LD100 of an oral dose of CCl4 was reduced by PB to an LD50, but the gentamicin pretreatment was without effect . When a sublethal dose of CCl4 was administered, both the SGOT and SGPT values were significantly lower in the PB group of rats . This biochemical protection was mirrored in the striking lack of histological liver necrosis in these animals, protection not shared by the gentamicin group or controls . The incidence of endotoxemia 24 hr after CCl4 as detected by lead acetate enhancement was also reduced by PB pretreatment . These findings further support the contention that endotoxins from the gut may be major contributors to the extent of liver injury induced by an unrelated toxin. Br J Dermatol, 1978 Aug, 99(2), 117 - 37 The pathogenesis of miliaria rubra . Role of the resident microflora; Holzle E et al.; Anhidrosis was induced in volunteers by covering the skin with an impermeable plastic film . The degree of sweat suppression and miliaria after a thermal stimulus was directly proportional to the increase in the density of resident aerobic bacteria, notably cocci . No anhidrosis resulted when antibacterial substances were used to prevent the expansion of the microflora . Histological study showed a PAS-positive diastase resistant amorphous mass deep within the acrosyringium after 2 days of occlusion, accompanied by a periductal dermal infiltration of leukocytes . After another 2 days the duct became clogged by an amalgam of degenerating leukocytes . This impaction sloughed after about 3 weeks as a result of epidermal renewal . Colonies of bacteria were never found within the ducts . It is postulated that cocci secrete a toxin which injures luminal cells and precipitates a cast within the lumen . Infiltration by leukocytes creates an impaction which completely obstructs the passage of sweat for several weeks. Br J Surg, 1978 Aug, 65(8), 560 - 4 Primary suture of the perineal wound following rectal excision for imflammatory bowel disease; Marks CG et al.; Delay in healing of the perineal wound is a major cause of disability in patients after excision of the rectum . The outcome of primary suture in 76 patients treated at St Mark's Hospital between 1967 and 1976 was correlated with a number of factors describing the patients, their preparation for surgery and details of surgical technique and management . The perineal wound healed by first intention in 33 patients . The remaining 43 patients regarded as failures included 7 with delayed breakdown after initial healing . The results showed that women fared better than men . Excision of the rectum following colectomy and ileostomy was associated with failure of the perineal wound to heal in 9 out of 10 patients . Treatments with peroperative ampicillin and topical antibacterial agents were both correlated significantly with success . Preoperative sepsis and operative contamination were followed by perineal sepsis and wound breakdown on 16 out of 21 occasions . Discriminant analysis showed that topical and peroperative antibacterial treatments, sex, preoperative sepsis and finally ACTH were the most important variables in descending order of importance . The prediction of success and failure by this procedure was 72.4 per cent correct. J Infect Dis, 1978 Aug, 138(2), 125 - 33 Antibacterial functions of macrophages in experimental protein-calorie malnutrition . I . Description of the model, morphologic observations, and macrophage surface IgG receptors; Keusch GT et al.; An experimental protein-calorie malnutrition was produced in weanling Sprague-Dawley rats . The model resembles human malnutrition with respect to weight loss, inanition, angular stomatitis, anemia, lymphopenia, hypoproteinemia with hypoalbuminemia, and marked thymic involution . In addition, systemic invasion by gram-negative rods was documented . However, no edema was produced, and animals did not survive for longer than six weeks on the protein-deficient diet . One percent glycogen was found to be a satisfactory nonprotein stimulus for induction of a peritoneal exudate consisting primarily of young macrophages . Electron microscopy showed that morphologic events of phagocytosis and degranulation proceeded normally in macrophages from protein-deficient animals . In addition, cell surface receptors for IgG were preserved under these experimental conditions . These data indicate that weanling rats may be employed as a small animal model for servere, fulminant protein-calorie malnutrition in humans. Antibiotiki, 1978 Aug, 23(8), 675 - 6 {Search for new antitumor antibiotics in the bleomycin group}; Gauze GF et al.; The culture of Penicillium avellaneum 444 and its bleomycin resistant variant may serve a rather valuable specific test for detecting organisms producing new antitumor antibiotics of the bleomycin group . The organisms producing antitumor antibiotics of the group of anthracyclines (rubomycin and carminomycin), actinomycins and other chemical groups do not inhibit the growth of these test-organisms . Such tests are also resistant to the effect of antibacterial antibiotics. Wien Klin Wochenschr, 1978 Jul 14, 90(14), 506 - 9 {Application of acerbine, a mixture of organic acids containing propylene glycol as lotion or ointment in paediatric surgery (author's transl)}; Geley L; Acerbine has been available for clinical trial since three years ago . Promotion of epithelialization, as well as antiphlogistic, antibacterial and fungicidal actions have been attributed to this preparation . This paper presents a critical appraisal of our own results with Acerbine; initial scepsis was soon dispelled by the evident efficacy of this preparation, both in the form of a lotion and ointment, and its wide scope of application . Moreover, our own studies revealed an excellent effect on keloids, which became smoother and visibly paler . A very good prophylactic and curative effect was observed in respect to all types of skin transplantation . So far Acerbine has been successfully applied in 117 patients who have completed their course of treatment . Acerbine is being currently employed in the case of 16 further patients who are still in hospital . No untoward side effects were recorded . Our findings confirm the opinion of other authors that hospitalization is shortened by the use of this preparation . The availability, more recently, of the new preparation in form of an ointment enables treatment to be continued on an ambulant basis or at home in many cases . Certain new fiies . The results of further explorative investigations into these aspects are under review at present. Antibiotiki, 1978 Jul, 23(7), 642 - 4 {Effect of inhalatory therapy with antibacterial preparations on the fungal-yeastlike flora of the respiratory tracts in pulmonary tuberculosis}; Kulik NM et al.; A total of 254 patients with various forms of the lung tuberculosis were examined on the presence of the yeast-like flora; 130 patients out of them (the main group) were subjected to complex antibacterial therapy including inhalation with antitubercle drugs and 124 patients (control) were not treated with inhalation . On acceptance to the stationary the fungal flora was registered in 22.4% of the patients including 20.9% of the males and 29.2% of the females . The fungi were found more often in old patients (33.3%), patients with diseases of long duration (29.7%) and patients with fibrous cavernous tuberculosis of the lungs (27.1%) . It was shown that the local treatment of the patients suffering from the lung tuberculosis with antitubercle drugs including streptomycin had no significant effect on either the period of the fungi carrying (22.3% before the treatment and 21.5% after the treatment, P less than 0.05), or development of the fungal diseases (1.9% in the main group and 1.6% in the control group, P greater than 0.05). Proc Natl Acad Sci U S A, 1978 Jul, 75(7), 3173 - 7 Oxygen-mediated heterogeneity of apo-low-density lipoprotein; Schuh J et al.; Mild oxidation of human serum low-density lipoprotein (LDL) converts the apoprotein from a nearly homogeneous component of high apparent molecular weight to a mixture of apparently lower molecular weight polypeptide components, as characterized by sodium dodecyl sulfate/polyacrylamide gel electrophoresis . This protein alteration, which correlates temporally with increases in the formation of lipid oxidation products and in the fluorescence of the apoprotein, is markedly reduced when oxygen is excluded or when EDTA or the free-radical-scavenging antioxidants, butylated hydroxytoluene or propyl gallate, are added . The conversion thus appears to be due to a reaction between the protein moiety and auto-oxidizing lipid . The presence of the antibacterial agent sodium azide markedly accelerates the oxidation, suggesting that it should only be used with caution in lipid-containing solutions. J Med Chem, 1978 Jul, 21(7), 639 - 43 Folate antagonists . 12 . Antimalarial and antibacterial effects of 2,4-diamino-6-{(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl}quinazolines; Elslager EF et al.; A series of 2,4-diamino-6-{(aralkyl and alicyclic)thio-, sulfinyl-, and sulfonyl}quinazolines was prepared via condensation of 5-chloro-2-nitrobenzonitrile or 5,6-dichloro-2-nitrobenzonitrile with the appropriate aralkyl or alicyclic thiopseudourea, reduction of the resulting 2-nitro-5-{(aralkyl or alicyclic)thio}benzonitrile with stannous chloride to the amine, and cyclization with chloroformamidine hydrochloride . Oxidation was effected with hydrogen peroxide or the bromine complex of 1,4-diazabicyclo{2.2.2}octane . These analogues when examined for suppressive activity against drug-sensitive lines of Plasmodium berghei in mice were not as active as 2,4-diamino-6-{3,4-dichlorobenzyl)amino}quinazoline (Ia). Arch Ophthalmol, 1978 Jul, 96(7), 1262 - 4 Efficacy of penicillin G, cefazolin, and gentamicin in M-K medium at 4 degrees C; Baum J et al.; Corneal-scleral shells are routinely stored in McCarey-Kaufman (M-K) medium at 4 degrees C . Antibiotics are added to the medium to suppress bacterial growth . We examined the antibacterial activity of penicillin G potassium, 100 microgram/ml, cefazolin sodium, 100 microgram/ml, and gentamicin sulfate, 20 microgram/ml against test organisms in M-K medium at 4 degrees, 23 degrees, and 37 degrees C for periods up to 18 hours . Within the limits of the experimental conditions, none of the antibiotics used could be relied on to sterilize an inoculum of sensitive bacteria in M-K medium at 4 degrees C, the recommended storage temperature. Arthritis Rheum, 1978 Jul-Aug, 21(6), 681 - 9 Hematologic and serologic studies in 6-sulfanilamidoindazole arthritis; Miller ML et al.; 6-sulfanilamidoindazole (6-SAI), an antibacterial sulfonamide, is known to cause an acute, self-limited inflammatory reaction in the hind paws of older rats . Administration of 6-SAI results in hyperfibrinogenemia which precedes the onset of clinical arthritis . The hyperfibrinogenemia is associated with the prolongation of dilute blood clot lysis times, appearance of heparin-precipitable fibrinogen, elevations in fibrin degradation products, and complement titers and serum electrophoretic pattern changes that consist of decreased albumin concentrations and increased beta globulin concentrations . Alterations in 6-SAI medicated young rats are less marked and require higher doses. Vet Rec, 1978 Jun 17, 102(24), 523 - 4 Distribution of trimethoprim/sulphadiazine in plasma, tissue and synovial fluids; Piercy DW; The subcutaneous implantation of tissue cages was used to study the distribution of trimethorprim and sulphadiazine into tissue (interstitial) fluid in calves, sheep and dogs over a 24-hour period . After oral dosing there was good gastrointestinal absorption of both antibacterial agents in dogs but only of the sulphonamide in sheep . The concentration of trimethoprim in tissue fluid peaked at five to seven hours after administration when it exceeded the plasma concentration . Sulphadiazine persisted in the plasma for longer than trimethoprim, but distribution into tissue fluid was slower . The findings show that reliance on plasma concentration curves alone in determinations of bioavailability of chemotherapeutic agents may lead to false interpretations. Can Med Assoc J, 1978 Jun 10, 118(11), 1395 - 8 Use of a topical antibiotic spray in vaginal surgery; Wright VC et al.; During vaginal hysterectomy with or without colporrhaphy a topical aerosol spray containing neomycin sulfate, polymyxin B sulfate and zinc bacitracin was used in 50 patients to decrease the change of postoperative pelvic infection; a placebo spray was used in another 50 patients . All patients were treated preoperatively with povidone iodine and postoperatively with nitrofurantoin and an antibacterial irrigating solution for the bladder if catheter drainage was necessary . The frequency of postoperative pelvic infection was 16% in the group sprayed with the antibiotic combination and 34% in the group sprayed with the placebo, a significant difference (P less than 0.05). Ciba Found Symp, 1978 Jun 6-8, (65), 285 - 94 The lactoperoxidase-thiocyanate-hydrogen peroxide antibacterium system; Reiter B; Lactoperoxidase present in various secretions oxidizes thiocyanate (SCN-) in the presence of H2O2 to an unstable oxidation product--hypothiocyanite (OSCN-), which is bactericidal for enteric pathogens including multiple antibiotic resistant strains of E . coli . The system damages the inner membrane causing leakage and cessation of uptake of nutrient, leading eventually to death of the organisms and lysis . The possible involvement of O2- and 1O2 is discussed. Farmaco {Sci}, 1978 Jun, 33(6), 438 - 52 {Reactions of potassium salts and methyl esters of some aroylhydrazino-carbodithioic acids}; Mazzone G et al.; In continuation of previous research designed to obtain compounds of pharmacological interest, the following substances were prepared, from the potassium salts (I-III) and from the methyl esters (IV-VI) of some aroylhydrazinocarbodithioic acids, derivatives of 1,3,4-oxadiazole (VII-XV), of 3-aminorhodanine (XVI-XVIII), of 1,2,4-triazole (XIX-XXI), of 7H-(1,2,4)-triazol{3,4-b} {1,3,4} thiadiazine (XXII-XXIV) and of 1,3,4-thiadiazole (XXV-XXX) . The compounds have present in the molecule a nucleus and radical which have produced marked biological activity in other series of compounds . To date some of the above compounds have shown antibacterial, antimycotic and antimitotic activity. J Antibiot (Tokyo), 1978 Jun, 31(6), 561 - 9 Diastereomeric 7-ureidoacetyl cephalosporins . II . 7beta {{{(Aminocarbonyl) amino}-2-thienylacetyl} amino}-7-methoxy-3-{{(1-methyl-1H-tetrazol-5-yl) thio} methyl}-8-oxo-5-thia-1-azabicyclo {4.2.0} oct-2-ene-2-carboxylic acid; Applegate HE et al.; The synthesis and antibacterial activity in vitro of 7-methoxylated cephalosporins having a thienylureidoacetyl or a thienylglycyl C-7 side-chain are described . Acylation of 7 beta-amino-7-methoxycephems with a novel 2-aminooxazolone hydrochloride under neutral conditions gave the thienylureidoacetyl derivatives in good yield with retention of configuration . 7 beta-{{D-{(Aminocarbonyl)amino}-2-thienylacetyl}amino}-7-methoxy-3-{{(1-methyl-1H-tetrazol-5-yl)thio} methyl}-8-oxo-5-thia-1-azabicyclo{4.2.0}oct-2-ene-2-carboxylic acid sodium salt (SQ 14,359) was found to have a broad-spectrum of antibacterial activity in vitro, particularly against beta-lactamase-producing organisms. Arch Intern Med, 1978 Jun, 138(6), 925 - 7 Mucormycosis . A complication of critical care; Agger WA et al.; Lethal nosocomial mucormycosis developed in three previously well individuals while they were receiving intensive care for acute hemorrhagic pancreatitis, for cardiogenic shock, and for a ruptured intra-abdominal aortic aneurysm . In two cases, the condition was first seen as progressive cavitary pneumonia refractory to antibacterial therapy; Mucoraceae was identified in all three patients only at autopsy . Each patient had received large doses of corticosteroids and broad-spectrum antibiotics, and all had suffered from respiratory failure, acute renal failure with acidosis, and severe hyperglycemia in association with total parenteral nutrition . Mucoraceae should be regarded as an additional nosocomial pathogen in the setting of advanced life-support care. Zentralbl Bakteriol {Orig B}, 1978 Jun, 166(6), 528 - 39 Studies on the mode of action of phenylmercuric borate on Escherichia coli . II . Biochemical localization and inhibition of some metabolic activities; Cortat M; The biochemical localization of phenylmercuric borate (PHB) on Escherichia coli shows that this disinfectant associates essentially with proteins . Protein electrophoresis demonstrates that each protein contains PHB, and that SH groups play a very important role in its fixation . The quantity of PHB able to associate with proteins is so large that many other electron donor groups must react with it . Moreover, it appears that concentration of PHB on cytoplasmic membrane results rather from the privileged position of this structure than from special physicochemical properties . The great reactivity of PHB towards proteins leads to numerous inhibitions and confers upon this antibacterial drug a very complex mode of action . Four important metabolic activities have been tested in the presence of PHB, namely: respiration, protein-synthesis, RNA synthesis and DNA synthesis . These four metabolic functions are rapidly and totally inhibited at low concentrations of PHB . The complexity of the mode of action of PHB makes the adaptation of bacteria to this disinfectant more difficult . In addition, in the case of plasmid dependent resistence, PHB, with its complexe mode of action, does not favour such a selection in opposition to the antibiotics which generally have a more specific mode of action. Oral Surg Oral Med Oral Pathol, 1978 Jun, 45(6), 947 - 54 The bactericidal potential of various endodontic materials for primary teeth; Cox ST Jr et al.; An in vitro study of the bactericidal or bacteriostatic effects of several pulp therapy compounds and their components on selected bacterial commonly isolated from infected primary teeth was undertaken . It was determined that zinc oxide had no inhibitory effects on E . coli, Staph . aureus, and Strep . viridans; however, the addition of eugenol to this system retarded the growth of only the grampositive organisms . The inclusion of zinc acetate as a setting accelerator inhibited both gram-positive and gram-negative bacteria . Also the inhibitory effects on these three organisms could be greatly enhanced by the addition of formocresol or paraformaldehyde to the zinc oxide--eugenol--zinc acetate system . It was also noted that Sargenti's N-2 paste was apparently no more effective in retarding growth of these organisms than the mixtures . Only the lead tetroxide and hydorcortisone present in the N-2 paste was toxic to the Staph . aureus but not to E . coli or to Strep . viridans . The other heavy metals in N-2 apparently have no antibacterial activity in the manner in which they were tested . This evidence suggests, but is not conclusive, that zinc oxide--eugenol--zinc acetate, with or without formaldehyde-containing compounds, may be effective in the elimination of bacteria from pulpotomized primary teeth . Therefore, the addition of highly cytotoxic chemicals which will remain sealed in a root canal and be active for extended periods of time may not be necessary for successful treatment. J Infect Dis, 1978 Jun, 137(6), 830 - 4 Probenecid and the antibacterial activity of cephradine in vivo; Kunst MW et al.; The influence of probenecid on the concentrations in blood and antibacterial efficacy of cephradine was studied in experimentally infected mice . An infection was induced by injection of 5 X 10(6) Escherichia coli into the thighs of irradiated, granulocytopenic mice . Probenecid was given 1 hr later, just before the administration of cephradine . The control animals received only the vehicle . Concentrations of cephradine in blood were determined for 2 hr; the antibacterial activity was estimated from bacterial counts made in the homogenized individual thighs . The blood concentrations of cephradine were 1.77 times higher in the probenecid-treated animals than in the controls . The potency ratio for doses was 2.41, the potency ratio for the areas under the drug concentration in blood vs . time curves was 1.34, and that for the peak blood concentrations was 1.43. Am J Med, 1978 Jun, 64(6), 933 - 6 Acidosis of synovial fluid correlates with synovial fluid leukocytosis; Ward TT et al.; The antibacterial activity of aminoglycoside antibiotics is significantly reduced by lowering the pH of the incubation medium . Since gram-negative septic arthritis responds poorly to aminoglycoside antibiotic therapy, we sought to determine whether synovial fluid acidosis contributes to this poor outcome . Synovial fluid samples from 22 patients with various forms of acute and chronic arthritis were examined for white blood cell count and pH . A close correlation (r = -0.92, p is less than 0.001) between an increasing white blood cell count and a decreasing pH was demonstrated . Since septic arthritis is associated with high white blood cell counts, in synovial fluid, the resultant low pH may contribute to the poor response to gram-negative septic arthritis treated with aminoglycoside antibiotics. Science, 1978 May 26, 200(4344), 902 - 7 Immunization against infectious disease; Mortimer EA Jr; Mortality and morbidity from infectious diseases in the United States have declined more than 90 percent since 1900 . Factors believed to be responsible for this decline include changes in the natural history of disease, sanitation, quarantine measures, control of nonhuman vectors, antibacterial drugs, and immunization . The contributions of each of these factors differ among the various infectious diseases; except for smallpox and diphtheria control, immunization had little effect until after World War II . The success of present and future immunization programs is endangered by public and physician complacency and by complex legal and ethical problems related to informed consent and responsibility for rare, vaccine-related injury. J Antibiot (Tokyo), 1978 May, 31(5), 441 - 50 Modification of seldomycin factor 5 at C-3'; Carney RE et al.; Attempted removal of the 3'-hydroxyl group of seldomycin factor 5 via displacement of a sulfonate ester has led to 3'-epi-seldomycin factor 5 . Removal of the hydroxyl group has been effected by the Barton procedure . The antibacterial activity of 3'-epi- and 3'-deoxyseldomycin factor 5 against various aminoglycoside-resistant strains is discussed. J Pharm Sci, 1978 May, 67(5), 706 - 9 Electronic structure--activity relationships of antibacterial acridines; Singh P et al.; The antibacterial activity of a series of amino- and fluorinated acridines was studied in the framework of their electronic structures . To calculate the electronic structure, a simple Huckel molecular orbital theory was used . A statistical regression analysis revealed linear correlations between the activity and the electronic indexes, particularly the electron density at the ring nitrogen. South Med J, 1978 May, 71(5), 512 - 5 Treatment of Nocardia asteroides infection with trimethoprim-sulfamethoxazole; Cook FV et al.; Although sulfonamide therapy has reduced the case fatality rate in infection due to Nocardia asteroides from nearly 100% to 25% to 45% there remains a need for a still more effective chemotherapeutic regimen . We describe three cases of serious infection due to N asteroides treated successfully with trimethoprim-sulfamethoxazole (TMP-SMX) and review an additional 15 cases from the world literature . Trimethoprim and sulfamethoxazole exhibit a synergistic interaction in vitro against N asteroides, and the agent reaches antibacterial concentrations in blood, lung, and the central nervous system . Clinical results have been satisfactory in the limited number of patients treated to date. J Med Chem, 1978 May, 21(5), 493 - 5 Mitomycin antibiotics . Synthesis of 7-methoxy-1-(N-pyrrolidino)mitosene and its methiodide; Mott J et al.; 7-Methoxy-1-(N-pyrrolidino)mitosene and its methiodide were synthesized . The latter compound was a potential bifunctional alkylating agent because of its two good leaving groups appropriately situated with respect to the indoloquinone chromophore . However, it was inactive in bacteriophage induction and P388 murine leukemia assays . Both compounds showed antibacterial activity in culture, and the former compound was very weakly active in inducing lysogenic bacteriophage. Pharmazie, 1978 Apr, 33(4), 196 - 8 Studies in potential organo-fluorine antibacterial agents . Part 1: Synthesis and antibacterial activity of some fluorinated arylsulfonylthiosemicarbazides and Arylsulfonylhydrazones; Joshi KC et al.; A series of fluorinated arylsulfonylthiosemicarbazides and arylsulfonylhydrazones has been synthesized . A representative number of the synthesized compounds have been screened for their antibacterial activity but none of the compounds showed significant activity. Pharmazie, 1978 Apr, 33(4), 184 - 5 The scope of the reactions of hydrazines and hydrazones . Part 4: Trisubstituted pyrazoles of possible hypoglycemic and antibacterial activity; Soliman R et al.; Condensation of ethyl 2,4-dioxo-6-phenyl hex-5-enoate (1) with 4-substituted sulphamyl phenylhydrazines (2) led to 1-aryl-3-ethoxycarbonyl-5-styrylpyrazoles (3) which on hydrolysis gave 1-aryl-5-styrylpyrazole-3-carboxylic acids (4) and upon permanganate oxidation gave 1-aryl-3-ethoxycarbonylpyrazole-5-carboxylic acids (5) . Similar condensation of hydralazine (6) with (1) gave the corresponding pyrazole (7) which on hydrolysis gave the acid 8. J Cell Sci, 1978 Apr, 30, 21 - 35 Ultrastructural localization of cationic proteins in human polymorphonuclear leukocytes; Brown WJ et al.; The present investigation is concerned with the use of the post-formalin ammoniacal silver reaction to detect the arginine-rich cationic proteins in human polymorphonuclear leukocytes at the ultrastructural level . These proteins appear to function as neutral proteases in antibacterial action and as mediators of inflammation . Originally, the ammoniacal silver reaction relied upon primary fixation in dilute formalin which prevented optimum fixation of tissues . This study shows that by using the proper sequence of glutaraldehyde fixation and the ammoniacal silver solution in conjunction with osmium tetroxide treatment, better fixation of the tissue and localization of the ammoniacal silver reaction can be achieved . Also, the ammoniacal silver reaction in human polymorphonuclear leukocytes is exclusively located in the large, crystalline cytoplasmic granules of eosiniphils . All other cytoplasmic granules of neutrophils, eosinophils, and basophils were found to be devoid of the ammoniacal silver reaction product . These results are contrary to previously published experimental data . Possible explanations for this discrepancy are discussed. Antibiotiki, 1978 Apr, 23(4), 317 - 21 {Experimental studies to set hygienic standards for benzylpenicillin in the air of a work area}; Shteinberg GB et al.; The character and level of benzylpenicillin toxic effect was studied in accordance with the methodic instruction for performance of the experiments on toxicological estimation and hygienic norms of antibiotics in the air of working areas in production premises . It was shown that the antibiotic was of low toxicity under conditions of a single exposure, did not cumulate and had no local irritating and resorbing effect . It was shown to be an allergen . Prolonged inhalation of benzylpenicillin in a concentration of 14 mg/m3 resulted in reversible changes in the function of the kidneys and liver of the animals, their sensitization and development of pronounced dysbacteriosis of the mouth and intestine mucosa . In a concentration of 1 mg/m3 benzylpenicillin had no general toxic and sensitizing effect but induced reversible changes in the normal autoflora . This allowed the authors to consider the above concentration to be maximum with respect to the antibacterial effect . On the basis of the experiments the maximum permissible norm (MPN) of the aerosol of benzylpenicillin disintegration was recommended at the level of 0.1 mg/m3. Am J Vet Res, 1978 Apr, 39(4), 633 - 8 Hemostatic function in swine as influenced by warfarin and an oral antibacterial combination; Osweiler GD; Pertinent literature on naturally occurring hemorrhagic diseases in poultry and livestock were reviewed and compared with reports on recent outbreaks of a hemorrhagic syndrome in swine . Epizootiologic, clinical, and hematologic data from porcine hemorrhagic disease suggest vitamin K-responsive hypoprothrombinemia . In weanling pigs, the toxicity of warfarin was compared with that in swine given tylosin and sulfamethazine antibacterial combination versus those given warfarin only . Toxicosis was induced in weanling swine fed warfarin daily at dose level of 0.055 mg/kg of body weight . Approximately 5 days after feeding was started, signs of poisoning appeared: lameness, anorexia, subcutaneous hematomata, melena, and periarticular enlargement . Administration of warfarin at dose level of 0.017 mg/kg did not cause clinical toxicosis, and 0.028 mg/kg produced significant increases in one-stage prothrombin time (OSPT) and activated partial thromboplastin time (APTT), but no evidence of clinical bleeding . When tylosin-sulfamethazine antibacterial combination was fed at normal and high dose levels concurrently with warfarin at dose level of 0.017 mg/kg of body weight, increase of clotting time, OPST, or APTT did not occur due to antibacterial influence . The antibacterial combination fed alone did not produce changes in clotting time, OSPT, APTT, fibrinogen, total protein, differential leukocyte count, or packed cell volume. J Parasitol, 1978 Apr, 64(2), 193 - 7 Evidence that sulfisoxazole, an antibacterial sulfonamide, can adversely affect the development of Brugia pahangi in Aedes aegypti mosquitoes; Jaffe JJ et al.; The average number of infective larvae recovered from Brugia pahangi-infected Aedes aegypti was approximately one-half that recovered from the controls after the former group of infected mosquitoes had ingested a 1.0% solution of sulfisoxazole diolamine (SXZ) in 10% sucrose-water for 4 consecutive days, beginning 4 days after infection . Most of the filarial larvae from the SXZ-treated mosquitoes were small and sluggish compared with those from the controls . There was no increased mortality of mosquitoes that ingested 1.0% SXZ in sugar-water for 4 days . Average filarial larval burdens were not decreased in mosquitoes that ingested a solution of 10(-6) M methotrexate (MTX), a potent dihydrofolate reductase inhibitor, in sugar-water for 4 days, beginning 4 days after infection . The distributional pattern of larval burdens in mosquitoes that ingested combined 1.0% SXZ and 10(-6) M MTX in sugar-water for 4 days closely resembled that seen in mosquitoes that had imbibed 1.0% SXZ only . Average filarial larval burdens were not decreased in mosquitoes with 4-day-old B . pahangi infections that fed upon jirds which received intraperitoneal injections of SXZ (2 g/kg) and MTX (1 mh/kh), alone and in combination, 1 hr previously . Survival of the mosquitoes that fed upon the drug-treated hosts was unaffected, as was the hatchability of their eggs and subsequent growth and development of the mosquito larvae. Zh Mikrobiol Epidemiol Immunobiol, 1978 Apr, (4), 31 - 7 {Natural antibodies (isohemagglutinins, heterophilic, antierythrocytic and antibacterial) in children with congenital immunologic deficiency syndromes}; Krizon SS et al.; Examination of 30 patients with immunodeficient diseases showed that the system of natural antibodies was considerably changed depending on the form and the extent of deficiency of the immune system: in agammaglobuinemia the antibodies under study were almost completely absent, and in immunological insufficiency with ataxia-teleangiectasis the production of antibacterial antibodies proved to be sharply decreased . The data obtained can be used both for the diagnosis of immunodeficiencies and for control of the restoration of the immunological competence after a number of therapeutic measures, particularly after the transplantation of the thymus-sternum complex. Ann Microbiol (Paris), 1978 Apr, 129(3), 265 - 84 Morphological mutants of Escherichia coli: nature of the permeability barrier in mon and envC cells; Starkova Z et al.; Morphological mon mutants and a chain-forming envC mutant of Escherichia coli K12 are hypersensitive to detergents and to various other antibacterial agents . Electron microscopy shows that the cytoplasmic membrane of growing mon and envC cells is dissolved by detergents, and that the cytoplasm dissociates into two parts of unequal density . The mutant envC is sensitive to actinomycin D and to rifampicin, is lysed by lysozyme in the absence of EDTA, and releases alkaline phosphatase in the absence of osomotic shock, indicating a gross perturbation of its outer membrane. J Pharm Pharmacol, 1978 Apr, 30(4), 236 - 9 The effect of various topical antibiotic and antibacterial agents on the middle and inner ear of the guinea-pig; Parker FL et al.; The topical application of antibiotics and anti-inflammatory agents is used to reduce inflammation of the middle ear mucosa and irradicate infection . Many of the antibiotic and anti-inflammatory preparations so used contain compounds known to be or are potentially ototoxic . Eighteen antibiotic, antibacterial, antifungal and anti-inflammatory compounds and four commonly used solvents were screened for the absence of ototoxicity and inflammation to the middle ear mucosa . All compounds were injected intra-tympanically and sensory hair cells loss recorded graphically . Inflammation of the middle ear mucosa was assessed macroscopically . Of the 18 compounds only three, penicillin, carbenicillin and nystatin were free of hair cell toxicity and inflammatory effects on the middle ear mucosa . Only one of the commonly used solvents was free of side effects. J Pharm Sci, 1978 Mar, 67(3), 413 - 5 S-(4-Chlorophenyl) 3-aryl-3-hydroxypropanethioates as antibacterial agents; Snyder HR Jr et al.; A series of S-(4-chlorophenyl) 3-aryl-3-hydroxypropanethioates was prepared and shown to have in vitro activity against several selected bacterial species. Antibiotiki, 1978 Mar, 23(3), 273 - 5 {Antibacterial therapy of liver abscesses of varying etiology}; Aliev VM; The investigation of microbial flora and its sensitivity in 196 patients with the kidney abscesses of various etiology showed expediency of the use of aminoglycosides, ampicillin and lincomycin . The local use of colloid iodine promoted rapid inhibition of the microbial flora . The dynamic observations showed an increase in the number of gramnegative pathogens by the 7th--10th day of the treatment . Rational surgical intervention, the antibiotic use with control of the microbial flora sensitivity, specific chemotherapy provided a decrease in the lethality up to 6.7 per cent. Antibiotiki, 1978 Mar, 23(3), 250 - 3 {Tetracycline hydrochloride complex formation with collagen}; Rudenko TG et al.; The quantitative indices and regularities of tetracycline hydrochloride binding with colelagen in the process of complex formation were studied in vitro . It was found that tetracycline-interacted with collagen . The amount of the antibiotic bound depended on its initial concentration in the mixture and the aggregate state of the protein: the amount of tetracycline hydrochloride absorbed by dissloved collagen was 10 times higher than that absorbed by polymerized collagen . The antibiotic bound with collagen did not lose its specific antibacterial activity. J Pharm Sci, 1978 Mar, 67(3), 380 - 3 Differences in antibacterial activity of benzalkonium chloride; Richards RM et al.; Benzalkonium solutions obtained from different manufacturers were shown to have different activities . This difference in activity was related to the composition of the benzalkonium chloride . The potential seriousness of this situation is emphasized, and a recommendation is made that the official monographs on benzalkonium chloride be amended appropriately, noting the apparently superior antibacterial activity of the tetradecyl (C14) homolog. Antimicrob Agents Chemother, 1978 Mar, 13(3), 479 - 83 Activity of flumequine against Escherichia coli: in vitro comparison with nalidixic and oxolinic acids; Greenwood D; The in vitro activity of the new antibacterial agent, flumequine, against Escherichia coli was compared with those of oxolinic acid and nalidixic acid . As judged by turbidimetric criteria, flumequine was considerably more active than nalidixic acid and slightly less active than oxolinic acid against both nalidixic acid-susceptible and -resistant strains . Resistance to all three drugs could be easily induced in vitro . The comparative efficacy of flumequine, oxolinic acid, and nalidixic acid was also tested in an in vitro model of the treatment of bacterial cystitis . In this system, suppression of bacterial growth was obtained with markedly lower concentrations of flumequine and oxolinic acid than of nalidixic acid, but prevention of the emergence of bacterial populations that exhibited increased resistance to these compounds depended on the maintenance of adequate drug levels. Farmaco {Sci}, 1978 Feb, 33(2), 142 - 7 Antibacterial activity and chemical reactivity of sulphanylamides . Rate constants of alkaline hydrolysis of N4-acetylsulphanylamides; Albasini A et al.; The alkaline deacylation rate constants of a collection of N4-acetylderivatives of acidic and non-acidic sulphonamides (SA) clearly show a definite trend due to the intramolecular effects induced by the different substitutions on the N1 nitrogen . The rate constant is interpreted as a reactivity index of the corresponding non-acetylated compound, and is found to be strictly correlated with the electron-availability of the p-amino group; thus providing an interesting correlation with the antibacterial activity of these drugs . Moreover, the reported experiments corroborate early predictions that the greatest reactivity of the p-amino group pertains to p-aminobenzoate (PAB) in the series of chemically related compounds, and that SA anions show the highest chemical and electronic resemblance to the essential metabolite (PAB); thus the high antibacterial activity of SA anions correctly corresponds to its close resemblance to the metabolite. Am J Vet Res, 1978 Feb, 39(2), 347 - 9 Relative efficacy of two oxytetracycline formulations and doxycycline in the treatment of acute anaplasmosis in splenectomized calves; Kuttler KL et al.; The efficacy of 3 antibiotic formulations was measured in the treatment of artificially induced anaplasmosis in the early stages of an ascending parasitemia (1% to 4%) in 23 splenectomized calves . Group 1, consisting of 5 calves, served as nontreated controls . Four calves (group 2) were treated 1 time with 10 mg of oxytetracycline (T-50)/kg of body weight IM; 5 calves (group 3) were treated 3 times with 10 mg of T-50/kg IM; 5 calves (group 4) were treated 1 time with 20 mg of an experimental oxytetracycline (T-200)/kg IM; and 4 calves (group 5) were treated 1 time with 10 mg of a synthetically derived antibacterial agent, doxycycline (D-100)/kg IM . All control calves died and 1 of 4 calves died that was treated 1 time with T-50 . Other deaths did not occur . All treatments were effective in moderating the infective process, but T-50 given 3 times and T-200 given 1 time were markedly more effective than T-50 and D-100 given 1 time . There appeared to be little or no difference in therapeutic efficacy between T-50 and D-100 given 1 time and between T-50 given 3 times and T-200 given 1 time. J Med Chem, 1978 Feb, 21(2), 221 - 5 Chemical modification of 1,4-diamino-1,4-dideoxy-3-O-(4-deoxy-4-propionamido-alpha-D-glucopyranosyl)-D-glucitol; Ponpipom MM et al.; Chemical modification of the 4'-N position of 1,4-diamino-1,4-dideoxy-3-O-(4-deoxy-4-propionamido-alpha-D-glucopyranosyl)-D-glucitol (GlA1) in the form of 4'-N-acyl analogues, e.g., 3, led to no significant potency enhancement . The n-propylamino analogue 4 was more active against gram-positive bacteria but was less act vs . gram-negative bacteria . The intrinsic activity of the 6'-chloro analogue 15 like the antibiotic GlA1 was not high, but the antibacterial spectrum was broad with moderate activity against most resistant organisms. J Pharm Sci, 1978 Feb, 67(2), 281 - 2 Synthesis and antibacterial evaluation of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles; Alaimo RJ et al.; The synthesis and antibacterial evaluation of a number of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles are described . The more active compounds against the test organisms in vitro generally were those substituted with halogens on the phenyl and benzothiazole rings. J Med Chem, 1978 Feb, 21(2), 189 - 93 Semisynthetic aminoglycoside antibacterials . 6 . Synthesis of sisomicin, Antibiotic G-52, and novel 6'-substituted analogues of sisomicin from aminoglycoside 66-40C; Davies DH et al.; The discovery of aminoglycoside 66-40C, a novel dimeric, unsaturated imine produced by Micromonospora inyoensis, afforded a versatile intermediate for the synthesis of a variety of sisomicin analogues modified at the 6' position . The conversion of 66-40C into sisomicin, antibiotic G-52, and a series of novel 6'-substituted analogues of sisomicin is described, and the biological activity of the products is discussed. J Dairy Res, 1978 Feb, 45(1), 109 - 18 Antibacterial effect of the lactoperoxidase system on psychotrophic bacteria in milk; Bjorck L; Activation of the antibacterial lactoperoxidase system in milk, i.e . increasing the thiocyanate concentration to 0.25 mM and adding an equimolar amount of H2O2, results in a substantial reduction of the bacterial flora and prevents the multiplication of psychrotrophic bacteria for up to 5 d . This treatment has no effect on the physico-chemical properties of milk and does not lead to the accumulation of resistant bacteria . The practical application of the lactoperoxidase system in prolonging the storage period of raw milk at low temperatures is discussed. Infect Immun, 1978 Feb, 19(2), 510 - 4 Humoral bactericidal systems: antibacterial potential of serum from young animals; Skarnes RC; The antibacterial potential of fresh serum obtained from young animals during a pre-antibody period of development was assessed against two smooth and two rough strains of gram-negative bacteria . The bactericidal capacity of serum from 3- to 4-week-old guinea pigs and 4- to 5-week-old rabbits was compared with that of serum from adults . Serum from young animals was deficient in natural antibodies, and in conventional dilution assays the bactericidal action was unimpressive, especially against the smooth strains . However, when decimal increments of bacteria were incubated in fresh undiluted serum, killing of both smooth and rough strains proved substantial . This finding may have particular meaning in the very young animal when natural antibodies are at ebb: cellular defense mechanisms may function less efficiently at this time and effect a greater reliance on humoral antibacterial systems. J Dent Res, 1978 Feb, 57(2), 171 - 4 Antibacterial activity of tooth-colored dental restorative materials; Orstavik D et al.; The antibacterial activity of dental restorative materials (12 resin based and one silicate) was tested in vitro against 5 species of bacteria . When fresh, all materials inhibited growth in pour plates of at least one bacterial strain . After storage in saline for 24 hours, the antibacterial activity was markedly reduced . There was a wide variation among the materials in the extent of their antibacterial activity . The bacterial strains apparently differed in their susceptibility to the antibacterial activity of the materials. Aktuelle Gerontol, 1978 Feb, 8(2), 85 - 91 Natural antibody level in old age; Batory G et al.; Antibacterial antibodies were determined with a passive hemagglutination micromethod using the Boivin extract of eight different strains of bacteria . Correlation between antibody values of different specificities and between the summarized titer values and individual antibody titers were found . A significant decrease in the average of the summarized titer values was observed especially for persons over 70 . The possibility of genetic regulation of normal antibody levels is suggested . The question whether the decrease in agglutinating antibody level in old age is due to the decreased activity of the corresponding immunocompetent cells or is secondary to other changes occuring in old age, is discussed. Ann Rech Vet, 1978, 9(2), 287 - 94 The effect of trypsin and chymotrypsin on the antibacterial activity of complement, antibodies, and lactoferrin and transferrin in bovine colostrum; Brock JH et al.; The effect of trypsin and chymotrypsin on antibacterial factors in bovine colostrum has been studied . Endogenous complement in colostrum was extremely sensitive to both enzymes . IgM was attacked by chymotrypsin but not by trypsin . Trypsin slowly attacked IgG1, causing loss of biological activity due to cleavage of both light and heavy chains . IgG1 was only very slightly attacked by chymotrypsin . Lactoferrin and transferrin in the iron-free state were both susceptible to proteolysis, but the iron saturated forms were more resistant and tended to give rise to stable iron-binding fragments. Chemotherapy, 1978, 24(6), 360 - 3 In vitro antibiotic sensitivity of Moraxella species; Rosenthal SL et al.; Minimal inhibitory concentrations of 17 antibacterial agents for 34 Moraxella strains were determined using a plate dilution method . A strain of Moraxella nonliquefaciens was found which produced beta-lactamase and was resistant to ampicillin and carbenicillin but not to cephalothin . Several strains were relatively resistant to erythromycin and sulfisoxazole . Disk sensitivity tests could be used to reliably predict penicillin and erythromycin resistance but not sulfisoxazole resistance. Acta Obstet Gynecol Scand, 1978, 57(4), 337 - 48 Ultrastructure and variations of human cervical mucus during pregnancy and the menopause; Chretien FC; Ultrastructural aspect and variations of cervical mucus have been studied by scanning electron microscopy in 58 pregnant and 29 menopausal women . In both groups, a striking tightening of the ultrastructural glycoprotein framework was demonstrated . The phenomenon appears to occur very rapidly at the beginning of pregnancy while patients near the menopause show more variable patterns . The results are compared to the known evolution of cervical mucus ultrastructure during the ovarian cycle and discussed from a rheological point of view . Particular attention was paid to the eventual antibacterial role of cervical mucus in pregnancy, which was found to be very plausible. Infection, 1978, 6(4), 171 - 4 The concentration of thiamphenicol in severely diseased human kidneys; Plomp TA et al.; The concentration of thiamphenicol in serum and renal tissue was determined in 17 patients with severly diseased kidneys after an intravenous injection of 1000 mg of the drug . Two hours after the administration the renal tissue concentrations ranged in patients with hydronephrotic kidneys from 38.0-63.5 microgram/g, in patients with cirrhotic kidneys from 17.9-42.7 microgram/g, in patients with pyonephrosis from 9.8-17.6 microgram/g and in patients with renal carcinoma from 37.7-64.2 microgram/g . The patient with the renal sarcoma had a level of 138.7 microgram/g . At the same time the serum concentration ranged from 4.6-15.2 microgram/ml . The highest renal tissue/serum concentration ratios of thiamphenicol were observed in patients with hydronephrotic kidneys and renal tumours, the lowest in cases of pyonephrosis . The influence of severe renal disease on the renal tissue/serum concentration ratios of thiamphenicol is discussed . The high renal tissue levels of thiamphenicol in patients with severely diseased kidneys fulfill an important condition for the antibacterial chemotherapy of kidney infections. Chemotherapy, 1978, 24(3), 121 - 33 Pharmacokinetics of cephalosporin antibiotics: protein-binding considerations; Singhvi SM et al.; The therapeutic activity of antibiotics depends on several factors including absorption, elimination kinetics, distribution in the body, minimal inhibitory concentrations (MIC), stability against enzymes, and plasma-protein binding . Some of these factors are interrelated, for example, the extent of protein binding of an antibiotic influences its elimination kinetics, distribution into tissues, MIC, and antibacterial activity . To evaluate the potential efficacy of an antibiotic, it is important to know the extent of its binding to plasma proteins especially since the protein-bound fraction of the antibiotic is devoid of antibacterial activity . Cephalosporins are a new class of broad-spectrum antibiotics that bind to plasma proteins in different degrees . Reported values for protein binding range from 6% for cephradine to 92% for cefazolin . The effects of protein binding of some of the commonly used cephalosporins on antibacterial activity and several pharmacokinetic parameters are discussed in this communication. Vestn Khir Im I I Grek, 1978 Jan, 120(1), 70 - 2 {Diagnosis and treatment of subphrenic abscess}; Parakhnoiak VI et al.; The clinical picture of subphrenic abscess taking place against the background of the treatment with modern antibacterial drugs has changed essentially, which requires a complex solution of the problem of the timely abscess diagnosis . The antistaphylococcal plasma and gamma globulin applied together with other methods of intense therapy proved to be the most effective after the dissection of the abscess. Infection, 1978, 6(1), 23 - 8 Assays of cephalosporin antibiotics administered prophylactically in open heart surgery . Determination of serum and tissue levels before, during and after cardiopulmonary bypass; Eigel P et al.; Twenty-eight patients who underwent open-heart surgery were divided into three groups, each of which received a different antibiotic from the cephalosporin series (cephalotin, cefazolin or cefamandole) in order to prevent infection . All antibiotics were given via intravenous infusion in a dosage of 2 g prior to surgery . To clarify the question of antibacterial activity under operative conditions with the cardiopulmonary bypass, the serum and tissue levels were determined before, during and after the surgical procedure . The effectiveness of the cephalosporins against bacteria most frequently encountered in open-heart surgery was demonstrated and substantiated by the serum and tissue concentrations . It became apparent that, in view of the favorable serum and tissue levels during and after the cardiopulmonary bypass, cefamandole should be considered the antibiotic of choice in preventing infections during open-heart surgery. J Antibiot (Tokyo), 1978 Jan, 31(1), 43 - 54 Chemical modification of some gentamicins and sisomicin at the 3''-position; Nagabhurshan TL et al.; Chemical and photochemical oxidative methods of de-N-methylation of some gentamicins and sisomicins at the 3''-position are described . Selective acetylation of gentamicins and sisomicins at the 1, 3, 2' and 6' and of gentamicin B at the 1, 3, and 6'positions are achieved by treatment of the free bases with carbon dioxide prior to acetylation . De-N-methylation of the above selectively blocked gentamicins and sisomicins followed by re-alkylation at the 3''-position and de-N-protection gives a series of 3''-N-alkyl analogues . The in vitro antibacterial properties of the new derivatives of gentamicins and sisomicins are given. J Pediatr, 1978 Jan, 92(1), 131 - 4 Oral antibiotic therapy for skeletal infections of children . I . Antibiotic concentrations in suppurative synovial fluid; Nelson JD et al.; To evaluate the feasibility of oral antibiotic treatment for pyogenic arthritis, one or more oral doses of antibiotics were substituted for the drugs being used for parenteral therapy . Synovial fluid and serum specimens obtained at randomized times after an oral dose of ampicillin, cephalexin, cloxacillin, dicloxacillin, or penicillin G were assayed for antibiotic content and antibacterial activity . Seventy specimens from 21 infants and children were studied . Peak synovial fluid concentrations were greater than 60% of peak serum concentrations with all drugs tested and there was adequate inhibitory activity against bacteria commonly causing arthritis . The degree of antibiotic binding to serum protein had no apparent effect on the degree of penetration into pyogenic synovial fluid. Chemotherapy, 1978, 24(1), 17 - 23 Tri-minocycline: a minocycline complex for parenteral use . I . Antibacterial activity and toxicity data; Kahan IL et al.; Aqueous solutions of tri-minocycline (equivalent to 20--50 mg/ml minocycline HCl) and preconstituted ready-for-use injections were prepared at the pH of blood; these exert high antibiotic activities equal to those of the parent substance . The chloroform/water distribution coefficients of tri-minocycline in the different types of injections were somewhat lower, but in the same order of magnitude as that of the parent substance . The MIC values of tri-minocycline proved to be very low and the LD50 values very high, their separation covering more than 3 orders of magnitude. Arzneimittelforschung, 1978, 28(9), 1602 - 4 {Experimental studies on topic application of amikacin to the eye (author's transl)}; Krasemann C et al.; The compatibility of amikacin as well as its penetration into the different tissues of the eye were studied experimentally in rabbits . Amikacin is well tolerated, both when applying drops and subonjunctival injections . When 1% solution of amikacin is dropped into the eye, antibacterially effective concentrations are achieved in the cornea and in the aqueous humour . There was only minimum penetration in the cornea found after subconjunctival injection . No amikacin was found in the vitreous body, neither when applying drops nor subconjuctival injections. Arzneimittelforschung, 1978, 28(8a), 1466 - 70 Pharmacological properties of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent; Mir GN et al.; 1-(2',6'-Dimethylphenyl)-3-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride), a potent, unique antidiarrheal agent, was tested for other pharmacological properties . It inhibited gastric acid secretion in both 4-h and 22-h pylorus-ligated rats and reduced mortality and gastric ulcer severity in the latter test . WHR-1142A also exhibited local anesthetic activity in the rabbit corneal reflex and guinea pig intradermal wheal tests and reverisbly blocked conduction in isolated frog nerves . Low doses of WHR-1142A increased plasma glucose concentration in fasted mice and rats and prolonged the hyperglycemia in response to a glucose meal . WHR-1142A showed mild diuretic activity but had no anti-inflammatory or antibacterial activity . The acute oral LD50 of WHR-1142A was 260 (208,328) mg/kg in male mice, 267 (212,336) mg/kg in male rats and 160 130,197) mg/kg in female rats. J Int Med Res, 1978, 6(2), 94 - 101 Antibacterial activity of sisomicin; Rossi A et al.; A study of the in vitro antibacterial activity of a new aminoglycoside, sisomicin, is reported . The results show no significant differences between the activity of sisomicin and gentamicin. Infection, 1978, 6(4), 166 - 70 Cefazolin and cephradine: relationship between serum concentrations and tissue contents in mice; Kunst MW et al.; The relationship between serum concentrations and tissue levels of various doses of cefazolin and cephradine was determined in experimentally infected mice . An infection was induced by injection of 5 X 10(6) Escherichia coli into the right hind leg, antibiotics were administered 1 h later . At 15-minute intervals mice were killed by exsanguination after a blood sample was taken, and the infected thigh was taken out and homogenized . The total amount of antibiotic per gram thigh muscle tissue was calculated on the basis of the concentration in the supernatant of the homogenate . From the parallel course between blood concentrations and total tissue contents it may be concluded that the thigh was easily accessible for both cephalosporins . The ratio between the total tissue content and the free serum concentrations was the same for both antibiotics despite the difference in protein binding between cefazolin and cephradine in mouse serum . This implies that the discrepancy between the relative antibacterial activity of the cephalosporins in vitro and in vivo found in earlier experiments cannot be explained by differences in accessibility of the tissue. Infection, 1978, 6(3), 140 - 3 Indications, interpretation and applications of antibiotic assays; Yourassowsky E; Routine monitoring of serum levels is imperative when antibiotics are given to patients with impairment of renal function . Other desirable indications include: need for assessment of adequate aminoglycoside levels in the initial management of severe infection; chloramphenicol therapy; need for control of bioavailability of new drugs or of new derivatives of known compounds; specific clinical situations (unexplained therapeutic failure, assessment of the oral use of antibiotics as an adequate therapy in patient with severe infections; appraisal of the innocuity of topical antibiotics in burned patients or in patients with liver or renal insufficiency) . The serum antibacterial test is highly recommended for assessing the adequency of antibiotic therapy in patients with bacterial endocarditis and in infected patients with impaired host resistance such as those with leukopenia . Control of initial treatment in any severe infection, osteomyelitis (particularly when combined antibiotics are used) and tuberculosis are other indications of this test . Any attempt to correlate the results yielded by antibiotic assays with in-vivo effectiveness must take into account the patient himself and the several unknown factors which, in each individual case, can affect the ultimate result of the antibiotic therapy, such as antibiotic delivery to tissues, drug binding to cellular debris, intracellular penetration of the antibiotic, etc. Antibiot Chemother, 1978, 23, 21 - 5 Yeast mutants with distorted cell membranes as a detection system for antitumor antibiotics; Gause GF et al.; Yeast mutants with distorted cell membranes, which are selectively inhibited by anticancer antibiotics and are not affected by antibacterial antibiotics, could be of considerable interest as test organisms . They could be used for the isolation of active antitumor substances from complex mixtures of natural compounds. J Clin Pathol, 1978 Jan, 31(1), 12 - 5 Specific and non-specific resistance to aminoglycosides in Escherichia coli; Mawer SL et al.; The turbidimetric responses of a strain of Escherichia coli K12 to gentamicin and tobramycin were investigated . Both agents showed antibacterial activity below the conventionally measured minimum inhibitory concentration, but exposure to such subinhibitory concentrations of either agent generated a bacterial population which was able to grow in previously inhibitory concentrations at a rate equivalent to that of the parent culture . The increase in resistance was non-specific in that both aminoglycosides were equally affected, and was unstable on multiple passage in drug-free broth . The response to tobramycin was unaffected by the presence of an R factor conferring gentamicin resistance, but exposure of the R factor bearing strain to gentamicin caused a concomitant increase in the resistance to tobramycin, apparently by a non-specific adaptive mechanism similar to that observed with the parent strain . It is suggested that prior treatment of a gentamicin-resistant organism with gentamicin (as may occur during blind therapy) may adversely affect the subsequent response to other aminoglycosides. Scand J Infect Dis Suppl, 1978, (14), 177 - 85 Antibiotics in bone tissues . Methodological and practical aspects; Dornbusch K; With regard to determination of antibiotic levels in bone, variance in results may be obtained as a consequence of type of the bones involved, degree of penetration of the drug used and of assay method performed . Measurements of antibacterial activity in bone from patients undergoing orthopaedic surgery were performed after preoperative treatment with doxycycline, lincomycin, clindamycin or cefuroxime . In performing the assay by the agar diffusion method, after extraction of the bone specimens in buffer according to classical systems, the concentrations of doxycyline were in the range of 0.05--0.6 microgram/g, clindamycin 0.4--4.9 microgram/g, lincomycin 1.7--2.9 microgram/g and of cefuroxine about 0.4 microgram/g . After electrophoresis in agarose-gel and followed by microbiological assay higher levels of these drugs were estimated possibly as a consequence of a diminution in the binding capacity of bone. Scand J Infect Dis Suppl, 1978, (14), 118 - 24 The tissue cage model in the distribution of antibacterial agents; Chisholm GD; Developments in the measurement of interstitial tissue fluid using the tissue cage model are described . The design and physical characteristics of tissue cages are examined and evidence is presented to show that the fluid contained within these cages is representative of interstitial tissue fluid . The distribution of a variety of antibacterial agents into tissue cage fluid is examined and shows that this technique is a reliable experimental model for the study of drug distribution . The results also show that some antibacterial agents may never, normally, distribute into the tissue fluid and that the use of tissue homogenates, especially the kidney, is unreliable as a guide to the tissue concentration of a drug. Scand J Infect Dis Suppl, 1978, (13), 37 - 46 On the pharmacokinetics of cephalosporin antibiotics; Andersson KE; A review is given on the pharmacokinetic characteristics of some cephalosporin antibiotics . The use of the pharmacokinetic parameters serum concentration, serum protein binding, serum half life, and apparent volume of distribution as a basis for the selection of the clinically most effective cephalosporin derivative is discussed . It is concluded that these parameters must be used in conjunction with data on tissue distribution to specialized sites, and with information on antibacterial activity and toxicity. J Dent Res, 1978 Jan, 57(1), 43 - 7 Alterations in lactoferrin in salivary gland disease; Tabak L et al.; During the active phase of chronic recurrent parotitis there is a marked elevation in the parotid concentration of lactoferrin (Lf), and iron-binding glycoprotein with antibacterial properties . The Lf concentration decreases during the recovery period, but still remains above normal levels . The changes of Lf in parotitis parallel recent findings in mastitis and pancreatitis . Elevations in Lf were also noted in five of six subjects with Sjogren's disease, but not in subjects with sarcoidosis, diabetes or "dry mouth" without sialographic changes . The source of the Lf has not been determined; it could arise in part from disrupting polymorphonuclear leucocytes and in part from epithelial cells that synthesize Lf in the salivary glands . Inflammatory stimulation of Lf synthesis would suggest a basic protective mechanism in exocrine glands and should be fully explored. Microbios, 1978, 21(85-86), 135 - 52 Cell composition and drug resistance in Escherichia coli; Hugo WB et al.; Resistance of micro-organisms to antibacterial drugs which cannot be attributed to a genetic change may often be traced to phenotypic changes in cell composition caused by differing growth conditions . To investigate an aspect of this attribute E . coli NCTC 86 was grown on a simple synthetic media containing alanine or cystine and, as a control, in nutrient broth . Cells grown on the media containing alanine and cystine showed a depleted total extractable lipid and phospholipid content . Phosphatidylethanolamine was notably reduced in both cases . Electrophoretic studies revealed a reduction in the surface lipid of cells grown on the simple synthetic media, while electron microscopy revealed defects in the cell wall of the cells grown on alanine . The total protein content of cells grown on alanine was reduced, whereas cells grown on the cystine showed an enhanced total carbohydrate content . Lipopolysaccharide synthesis was possibly also affected as judged by 2-keto-3-desoxy-D-manno-octonic aid content . The action of p-tertiary amylphenol, cetrimide and polymyxin B sulphate, showed that cells grown on the media containing alanine were most susceptible to the action of the phenol and cetrimide, whilst cells grown on the media containing cystine were most resistant to the action of polymyxin. J Int Med Res, 1978, 6(1), 72 - 7 The effectiveness of topical antibacterials in acne: a double-blind clinical study; Franz E et al.; In a double-blind study, three groups of patients with mild to moderate acne were treated for eight weeks with topical acne creams containing the antibacterials triclosan or triclosan plus propylene phenoxetol . The formula without antibacterials served as the control . Total-face lesion counts, evaluation of the overall degree of inflammation of the lesions, and patient self-assessment showed the added efficacy of the antibacterials when incorporated into the control. Folia Microbiol (Praha), 1978, 23(6), 438 - 43 Eurotium (Aspergillus) repens metabolites and their biological activity; Podojil M et al.; Eurotium repens mycelium cultivated under static conditions was used to isolate and identify metabolities--echinulin, physcion, erythroglaucin, flavoglaucin and asperentin; the filtrate of the culture yielded asperentin 8-methylether . The broadest biological activity spectrum was displayed by asperentin which had antibacterial and antifungal effects and, at a concentration of 86 microgram/ml, caused 50% mor7 tality in Artemia saline larvae . The highest cytotoxicity towards HeLa cells was found in physcion which caused 50% growth inhibition at a concentration of 0.1 microgram/ml. Acta Microbiol Pol, 1978, 27(1), 63 - 71 Primary production and extracellular release by phytoplankton in some lakes of the Masurian Lake District, Poland; Chrost RJ et al.; The primary production and extracellular release by phytoplankton were measured at different depths of Mikolajskie Lake, Rynskie Lake and Beldany Lake (Masurian Lake District, Poland) . The release of dissolved organic compounds was found to be related to the rates of primary production . The percentage of extracellular release (PER) of organic matter in the photic zone showed an inverse relationship with particulate production and chlorophyll alpha concentration . The highest PER was determined in the epilimnion of the studied lakes, where also increased release was observed . The higher release of algal products of photosynthesis in the photic zone than in the profundal is probably caused by the inhibition of physiological activity of bacteria by antibacterial substances produced by algae . The substances released by algae in the profundal are taken up by aquatic bacteria which explains the lower release and PER measured. Ann Anesthesiol Fr, 1978, 19(11-12), 909 - 13 {Postoperative peritoneal irrigation in generalized peritonitis treated in an intensive care unit}; Manelli JC et al.; Over a period of four years, 16 patients with generalized peritonitis have been treated by postoperative peritoneal irrigation in an Intensive Care Unit . The majority of cases involved postoperative peritonitis accompanied by severe visceral failure . The irrigation liquid, containing an antibacterial agent, was perfused for between one and eleven days at a high flow rate (mean 16.5 I) . The overall mortality in the series was extremely high (75 p . 100), and even greater (85 p . 100) if only the cases of postoperative peritonitis were considered . Anatomical examination of the peritoneum, performed on reintervention or at autopsy, revealed an abnormally high incidence of residual abscesses . These are responsable for the continuation or recurrence of infection, and explain the high mortality . These observations, combined with the frequent occurrence of local or general complications, led the authors to reject peritoneal irrigation in postoperative peritonitis in the presence of severe visceral failure, and to use it, in selected cases, only for periods not exceeding 48 hours. Biochemistry, 1977 Dec 13, 16(25), 5573 - 8 Neocarzinostatin: effect of modification of side chain amino and carboxyl groups on chemical and biological properties; Samy TS; The antitumor protein neocarzinostatin (NCS), isolated from Streptomyces carzinostaticus, is a single chain polypeptide with 109 amino acid residues . Complete acylation of the amino groups (alanine-1 and lysine-20) was observed when NCS was allowed to react with 3-(4-hydroxyphenyl)-propionic acid N-hydroxysuccinimide ester at pH 8.5 . Since the ensuing bis{(alanine-1, lysine-20)-3-(4-hydroxyphenyl)}-propionamide NCS was fully active in antibacterial potency and in the inhibition of growth of leukemic (CCRF-CEM) cells in vitro, it appears that the two amino groups in the protein are not essential for biological activity . Radiolabeled NCS was prepared by using a tritiated or 125I-labeled acylating agent . Since the CD spectra of native and bis(alanine-1, lysine-20)-amino modified NCS were indistinguishable, there is presumably no change in the native conformation of the protein due to acylation . Reaction of NCS with ammonium chloride in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide at pH 4.75 converted all the 10 carboxyl groups into carboxamides and produced a protein derivative of basic character . This modification caused a change in the native conformation of the protein accompanied by a loss in biological inhibitory activities. J Med Chem, 1977 Dec, 20(12), 1665 - 8 3-(3-Substituted prop-1-enyl)cephalosporins; Beeby PJ et al.; The synthesis of cephalosporin derivatives possessing a 3-substituted prop-1-enyl group at the 3 position is described . This was achieved using the reaction of vinylmagnesium chloride with the 3-formyl derivatives 1 to give a vinylcarbinol which readily underwent allylic rearrangements to give the desired side chains . The new derivatives exhibited potent in vitro and in vivo antibacterial activity. Inflammation, 1977 Dec, 2(4), 295 - 307 Steroids, aspirin, and inflammation; Katler E et al.; The ability of adrenal corticosteroids to both both suppress inflammation and compromise host defenses has been well documented . Recently, a series of in vitro and in vivo experiments, based on our new knowledge of the cell biology of inflammation and the biochemistry of the phagocytic cell itself, has provided new insights into the mechanism of steroid action in the inflammatory process . Evidence is presented that pharmacologic doses of steroids are capable of inhibiting each of the steps in phagocytic-micro-organism interaction: chemotaxis, recognition and opsonization, phagocytosis, membrane fusion, and degranulation . In addition, steroid alteration of the postphagocytic superoxide production, hydrogen peroxide generation, and prostaglandin and thromboxane synthesis is described . The antiinflammatory effects of aspirin and indomethacin can be explained almost entirely by virtue of their ability to inhibit cyclooxygenase, this preventing the transformation of arachidonic acid to both prostaglandins and thromboxanes . The cortisol-induced inhibition of endoperoxides, prostaglandins, and thromboxanes (at a site proximal to the release of arachidonic acid) may well explain those antiinflammatory actions that cortisone shares with aspirin . However, patients treated with nonsteroidal antiinflammatory agents effectively combat infections . In contrast, corticosteroids have more profound effects, as can be seen by the inhibition of superoxide production, with the subsequent decrease in hydrogen peroxide generation and the diminution in release of the antibacterial lysosomal hydrolases within the phagocytic vacuole . Thus, corticosteroids interfere with the killing of microorganisms . This new understanding of the pharmacologic action of cortisol on phagocytic cells explains, we believe, how glucocorticoids alleviate inflammation while, at the same time, they permit multiplication of the offending microorganism within the phagocyte. Nord Vet Med, 1977 Dec, 29(12), 533 - 8 Studies of the pathogenesis of enteric E . coli infections in weaned pigs . The significance of the milk of the dam in preventing the disease; Svendsen J et al.; Milk from sows whose progeny developed post weaning E . coli diarrhoea (PWD milk) and from sows which were immunized by intramuscular vaccination using a homologous strain of E . coli (immune milk) were tested in ligated segments of pig intestine . The results showed that PWD milk neutralized the enterotoxigenic, fluid accumulating capacity of the lysate of the disease-causing E . coli pathogen . A similar effect was seen by using immune milk (Table I) . Neither PWD milk nor immune milk contained sufficient antibacterial activity to neutralize the fluid accumulating capacity of live cultures of E . coli O149:K91, while such activity was contained in immune serum . It is concluded that milk from sows whose progeny developed PWD contains antibodies capable of neutralizing the enterotoxigenic effects of the homologous E . coli organisms . It is suggested that the presence in milk from these sows of antibody-mediated activity against enteropathogenic E . coli organisms may be instrumental in preventing the disease in the progeny during the suckling period and consequently, when this protective milk supply stops at weaning, the disease may develop in susceptible animals, mainly because their own production of specific E . coli antibodies is insufficient to prevent PWD. J Med Chem, 1977 Dec, 20(12), 1592 - 4 Studies of antitumor agents . 1 . Resolution of racemic 1-(tetrahydro-2-furanyl)-k-fluorouracil into the R and S isomers and examination of the biological activities of the isomers; Yasumoto M et al.; 1-(Tetrahydro-2-furanyl)-5-fluorouracil (Thf-FU), which is named Ftorafur or FT-207 and is used clinically as an antitumor agent, was conveniently synthesized by condensation of the trimethylsilyl derivative of 5-fluorouracil with 2-acetoxytetrahydrofuran using NaI as a catalyst . This optically inactive Thf-FU was resolved into optically active (R)-(+)- and (S)-(-)-Thf-FU in high optical purity and excellent yield by formation of diastereoisomers with brucine . 13C NMR data were obtained on Thf-FU and related compounds and the antibacterial activities and in vivo antitumor activities of these isomers were tested . The degradations of these isomers to 5-fluorouracil by liver microsomes were also examined . No significant differences were found in any of these properties of these isomers. Farmaco {Sci}, 1977 Dec, 32(12), 909 - 22 Structure-activity correlations for antibacterial 1,5-benzodiazepine derivatives on gram-positive cells; Grieco C et al.; The antibacterial activity of a set of 1,5-benzodiazepine derivatives against Staph, aureus and Strep, pyogenes has been correlated with structural features of the compounds examined . It is shown by means of substituent constants and regression analysis that the lipophilic character of the molecule is the most important factor in determining its activity . Electronic and steric effects appear to be quite important. J Dent Res, 1977 Dec, 56(12), 1599 - 602 Alkylamine salts and amides: in vitro inhibition of S mutans 6715; Warner VD et al.; Our studies with the salts and amides of alkylamines have shown that the undecylenate salts have significant in vitro activity against S mutans No 6715, suggesting that these agents are worthy of additional evaluation . The attempt to increase activity by combining undecylenic acid with the alkylamines was not successful; however, better attachment to tooth surfaces and/or retention during washing did occur . Our results suggest that the free amino group of alkylamines and the free acid group of undecylenic acid are required for these two classes of agents to demonstrate antibacterial activity. Drugs, 1977 Dec, 14(6), 401 - 19 Vitamin A acid: a review of its pharmacological properties and therapeutic use in the topical treatment of acne vulgaris; Heel RC et al.; Vitamin A acid (retinoic acid: tretinoin) is a vitamin A derivative used in the topical treatment of acne . It acts by 'unseating' comedones, improvement developing slowly over a period of 2 to 3 or more months, and is also said to prevent the formation of new lesions . About three-quarters of patients with acne vulgaris benefit from treatment . In controlled studies, results achieved after a 3 to 4 months course of treatment were superior to those with sulphur-resorcinol-salicylic acid . When compared with benzoyl peroxide, results were variable and appear to depend on the length of treatment, the types of formulations used, and the concentrations compared . Application of vitamin A acid should be continued until the patient has been free of new lesions for several months . Further continued application at a less frequent interval or using a less active dosage form may help to prevent exacerbations of acne . A systemic antibacterial agent such as tetracycline can be given as well as in patients with moderate to severe lesions . Vitamin A acid is used in conjunction with gentle washing (to remove surface oil) but should be applied to a dry skin to avoid unnecessary irritation . Patient education and encouragement are crucial during the initial phase of treatment when microcomedones may be converted to pustules prior to desquamation. J Pharm Pharmacol, 1977 Dec, 29(12), 717 - 22 Loss of antibacterial preservatives from contact lens solutions during storage; Richardson NE et al.; The preservative content of 34 commercially available contact lens solutions has been determined . Over half of the solutions contained less than 90% of the stated preservative content . Storage tests conducted at 40 degrees, using both simulated and commercially available contact lens solutions in plastics containers of the type used to present these products showed that thiomersal and chlorbutol appeared to be sorbed by these containers in contrast to benzalkonium chloride and chlorhexidine gluconate which interacted mainly by a surface adsorption process . The extent of any interactions was dependent upon the type of plastics material used to fabricate the container. C R Acad Sci Hebd Seances Acad Sci D, 1977 Nov 14, 285(13), 1215 - 7 {Description of some simple tests allowing the distinction between bacteriocins sensu stricto and other antibacterial agents produced by bacteria}; Hamon Y et al.; In contrast with other antibacterial agents produced by bacteria, the bacteriocins of Gram -- bacteria (briefly: cins G--) are characterized by their primary lethal action, their inactivation by trypsin, their resistance to pH 2 (in the crude state) and insensitivity to DNase I after treatment with 7 M urea . Only 4 among 26 studied cins G + have the 4 above-cited properties and share most properties of cines G--. J Pharm Sci, 1977 Nov, 66(11), 1607 - 11 N-Glucopyranosyl-5-aralkylidenerhodanines: synthesis and antibacterial and antiviral activities; Foye WO et al.; A series N-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-5-aralkylidenerhodanines was synthesized, and the acetyl groups were removed to give N-beta-D-glucopyranosyl-5-aralkylidenerhodanies without cleavage of the rhodanine ring by means of acid hydrolysis . Alkaline hydrolysis with ammonia in methanol resulted in cleavage to N-glucosylthiourea, providing evidence for N-glycoside formation . A number of the rhodanine derivatives, especially those with nitro or chloro groups in the aromatic ring, showed antibacterial activity . N-beta-D-Glucopyranosyl-5-(4-nitrobenzylidene) rhodanine showed antiviral activity by inhibition of viral RNA synthesis . Some effect on blood sugar levels also was observed with several rhodanines. J Med Chem, 1977 Nov, 20(11), 1445 - 8 Antibacterial halogenoacetyl derivatives of amino acids and simple peptides; Goodacre J et al.; The vital role of D-alanine and L-lysine in the peptidoglycan crosslinking process in the bacterial cell wall prompted preparation of various small peptides incorporating these amino acids . N-Iodoacetyl or -bromoacetyl derivatives of the peptides were then prepared in the hope that they would serve as active-site-directed irreversible inhibitors of cell wall transpeptidases . Certain of the halogenoacetyl dipeptide esters, but not the corresponding free acids, showed slight antistaphylococcal activity . Subsequent structural variation showed that inclusion of C-alanine or L-lysine was not necessary, since antibacterial activity was at least as good when the dipeptide unite was replaced by glycylglycine or by an omega-aminoalkanoic acid . It was concluded that the observed antibacterial activity was probably not due to specific inhibition of a cell wall transpeptidase. Acta Otolaryngol, 1977 Nov-Dec, 84(5-6), 440 - 5 Maxillary sinusitis . Effects of treatment on the local antibacterial defence; Carenfelt C; Low levels of immunoglobulins and complement in purulent antral secretion might jeopardize the local antibacterial defence . To evaluate whether or not antibiotic treatment and antral drainage influence the local content of immunoglobulins and complement, samples of secretion were analysed both prior to drainage and 1-2 days after drainage . In those patients requiring repeated drainage for their recovery, the local concentration of IgA and IgG was significantly lower in the secretion obtained prior to drainage than the local concentration found in patients who recovered after the initial drainage . It was also demonstrated that after drainage, the level of IgA, IgG and the complement factors C3 and C4 increased significantly, whereas the proteolytic activity in the secretion usually decreased. J Antibiot (Tokyo), 1977 Oct, 30(10), 843 - 6 Synthesis and antibacterial activities of 1-N {(S)-omega-amino-2-hydroxyalkyl} kanamycin A derivatives; Richardson K et al.; Four 1-N-aminohydroxy-alkyl derivatives of kanamycin A were prepared and their in vitro activities against aminoglycoside-sensitive and aminoglycoside-resistant organisms were compared with amikacin . 1-N-{(S)-4-Amino-2-hydroxybutyl} kanamycin A (Fig . 1, compound 2, code no . UK-18,892) was equipotent to amikacin in all these tests and in mouse protection studies. J Antibiot (Tokyo), 1977 Oct, 30(10), 836 - 42 The aminoglycoside antibiotics . I . Synthesis and biological evaluation of an analog of gentamicin; Sitrin RD et al.; The synthesis of 2-deoxy-4-O-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-D-erythrohexopyranosyl)-6-O-(3-deoxy-3-methylamino-alpha-D-xylopyranosyl)-D-streptamine (1), an analog of gentamicin A, from diideoxyneamine and methyl 3-methylamino-3-deoxy-beta-D-xylopyranoside is described . The product was characterized by its 13C nmr spectrum and was found to exhibit broad spectrum antibacterial activity. J Antibiot (Tokyo), 1977 Oct, 30(10), 779 - 88 Tallysomycin, a new antitumor antibiotic complex related to bleomycin . I . Production, isolation and properties; Kawaguchi H et al.; The unusual actinomycetes strain No . E465-94 produced a complex of new glycopeptide antibiotics tallysomycin, which was separated by CM-Sephadex chromatography into two major components, A (C68H107N21O27S2) and B (C62H95N19O26S2) . They were isolated first in a copper-chelated form and showed physico-chemical properties similar to those of the bleomycin-group of antibiotics . Tallysomycin exhibited broad antibacterial and antifungal activity, and was highly active in vivo against bacterial infections in mice . Tallysomycins A and B demonstrated potent activity in the prophage induction of lysogenic bacteria. Arch Dis Child, 1977 Oct, 52(10), 778 - 81 Intramuscular iron-dextran and susceptibility of neonates to bacterial infections . In vitro studies; Becroft DM et al.; An increased incidence of E . coli sepsis has been observed in neonates given intramuscular iron-dextran for prevention of iron deficiency . Mechanisms for this apparent effect on susceptibility to infection were investigated by comparing phagocytic and antibacterial functions in paired samples of venous blood from 7 infants, median age 5 days, before and after iron-dextran . Post-treatment sera had increased inhibitory effects on leucocyte chemotaxis and markedly reduced bacteriostatic effects agaainst E . coli . The clinical relevance of the effects on chemotaxis is uncertain . The reduction in serum bacteriostasis is similar to that observed in other forms of hyperferraemia not associated with saturation of transferrin, and is a likely cause of the increased susceptibility to infection in vivo . We consider that prophylactic treatment with parenteral iron-dextran is contraindicated in early infancy. Surg Clin North Am, 1977 Oct, 57(5), 1089 - 1102 The diabetic foot: an alternative approach to major amputation; Robson MC et al.; Of the complications of diabetes mellitus, none is more devastating than gangrene of the foot and the threat of leg amputation . The pathophysiology of vascular insufficiency, neurotrophic changes, and infection leading to this gangrene have been reviewed . Based on this pathophysiology, an approach for conservative surgery of the diabetic foot has been outlined . Using known principles of wound healing and the management of soft tissue infection, obviously necrotic or infected tissue is debrided and the wound managed conservatively . The use of debriding adjuncts such as the pulsating jet lavage, topical antibacterials, and biologic dressings are suggested to control the infection so that the wounds can be closed with either skin grafts or local flaps . This method can result in salvage of many feet and the maintenance of biped ambulation since the outlook for the diabetic with a major amputation is markedly different from the nondiabetic amputee. J Med Chem, 1977 Oct, 20(10), 1287 - 91 Synthesis and antibacterial activity of some derivatives of tolypomycinone . Relationship between structure and activity in ansamycins; Bellomo P et al.; 3-Aminotolypomycinoes and 3,16-diamino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to tolypomycinone, obtained by mild hydrolysis of the antibiotic tolypomycin Y.3-Amino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to 16,17-dihydrotolypomycinone . In vitro microbiological tests showed high antibacterial activity in compounds obtained by the addition of primary amines, which must be unbranched in the alpha position to the nitrogen atom to position 3 of the naphthoquinone ring . The relationship between structure and activity is described, and evidence is presented that hydrogen bonding between the amino NH bonded to C3 and the amide CO of tolypomycinone is very important for biological activity. J Periodontol, 1977 Oct, 48(10), 646 - 9 Prolongation of antibacterial activity of chlorhexidine adsorbed to teeth . Effect of sulfates; Turesky S et al.; The results suggest that the effectiveness of sulfates in prolonging the antibacterial activity of teeth treated with chlorhexidine gluconate is related to the acidity and concentration of the sulfate solutions . The acidity may contribute to the effectiveness by modifying the tooth surface for enhanced reaction with sulfate ions . It is suggested that during the priming process bonded crystals of calcium sulfate develop which become transformed by treatment with chlorhexidine gluconate to relatively insoluble chlorhexidine sulfate. Arch Dermatol, 1977 Oct, 113(10), 1390 - 1 Topical clindamycin in acne vulgaris . Safety and stability; Algra RJ et al.; Eighteen patients with acne vulgaris used a hydroalcoholic solution of clindamycin hydrochloride topically . Serum samples were obtained and assayed for clindamycin; no evidence for systemic absorption was found . The clindamycin capsules used in this preparation contained insoluble fillers that may be removed by filtration without loss of in vitro antibacterial activity . This solution is stable for at least six months. J Antibiot (Tokyo), 1977 Sep, 30(9), 705 - 13 Cephalosporins . III . 7-(O-Aminomethylphenylacetamido)cephalosporanic acids with bicyclic heteroaromatics in the C-3 side chain; Naito T et al.; Bicyclic heteroaromatic thiols with a bridge-head nitrogen atom were used for nucleophilic substitution of 7-ACA at the C-3 acetoxy function followed by N-acylation of the 7-amino group with o-aminomethylphenylacetic acid to afford a series of new cephalosporins (24) with potent antibacterial activity against gram-positive and gram-negative organisms . The most active member of this series was 7-(o-aminomethylphenylacetamido)-3-(tetrazolo-{4,5-b}pyridazin-6-ylthiomethyl)-3-cephem-4-carboxylic acid (BB-S 226) (24e) with antibacterial activity superior activity superior to cephalothin and cefazolin. J Antibiot (Tokyo), 1977 Sep, 30(9), 698 - 704 Cephalosporins . II . 7-(O-Aminomethyl-phnylacetamido) cephalosporanic acids with six membered heterocycles in the C-3 side chain; Naito T et al.; 7-(o-Aminomethylphenylacetamido)cephalosporanic acids with six-membered heterocycles in the C-3 side chain were prepared by nucleophillic substitution of 7-ACA at the C-3 acetoxy group followed by N-acylation of the 7-amino group . The 7-side chain acid, o-aminomethylphenylacetic acid (5), was prepared by two new convenient routes, which involved Schmidt reaction of indanone (2) followed by cleavage of the lactam ring or reduction of o-cyanophenylacetic acid (10) starting from o-nitrotoluene . The antibacterial activity of the cephalosporins in this series depends on the heterocycle in the C-3 side chain . In general pyridazines gave cephalosporin derivatives possessing better activity than those with a pyridine or pyrimidine ring . The most active member of the new cephalosporins was 7-(o-aminomethylphenylacetamido)-3-(6-hydroxypyridazin-3-ylthilmethyl)-3-cephem-4-carboxylic acid (BB-S 150) (1g) which has in vitro antibacterial activity superior to cephalothin and cefazolin against both gram-negative and gram-positive organisms . The in vitro activity of BB-S 150 determined in mice was superior to cephalothin and comparable to cefazolin. Vestn Khir Im I I Grek, 1977 Sep, 119(9), 12 - 4 {Puncture method of treating amebic abscesses of the liver}; Tikhii AT; In surgical treatment of hepatic amebic abscesses by means of extensive dissection and drainage the postoperative lethality remains high . The literature data and the author's own observations on 30 patients, who underwent puncture of amebic abscess of the liver together with specific and antibacterial therapy, which resulted in their recovery, permit to consider paracentensis as a method of choice, when there are no complications, such as a purulent discharge into the adjoining organs and tissues, which calls for surgical intervention. Antibiotiki, 1977 Sep, 22(9), 829 - 32 {Methodological bases for the hygienic standardization of antibiotics}; Shteinberg GB et al.; For determination of the maximum permissible concentrations of antibiotics it is necessary to develop some specific approaches conditioned by the peculiarities of the biological effect of antibiotics in addition to the use of the general principles of the hygienic rationing of the factors of the production environment . It is advised to determine the thresholds of the specific antibacterial and allergen effect of antibiotics in the acute experiment in addition to the threshold of the general toxic effect. Nord Vet Med, 1977 Sep, 29(9), 369 - 75 Effect of vaccination of sows with Bordetella bronchiseptica on the incidence of atrophic rhinitis in swine; Pedersen KB et al.; Vaccination of pregnant sows with Bordetella bronchiseptica was performed in an SPF herd with clinical atrophic rhinitis . Agglutinins against the organism were induced in serum and colostrum by the vaccination . The antibody titres were generally higher in colostrum than in corresponding serum samples . The frequency at slaughter of turbinate atrophy (+, ++, +++) was lower among pigs from vaccinated sows (11%) than in pigs borne by unvaccinated sows (20%) . In the control group a lower daily weight gain was observed in pigs with turbinate atrophy than in pigs with normal noses . The mean daily weight gain in pigs with turbinate atrophy borne by vaccinated sows was slightly lower than in pigs without atrophy of conchae, but the difference was not significant . A specific immunological prophylaxis might be an alternative to antibacterial treatment in herds where atrophic rhinitis is aetiologically related to B . bronchiseptica infection. J Pharm Sci, 1977 Sep, 66(9), 1312 - 6 Thermal decomposition of amorphous beta-lactam antibacterials; Pikal MJ et al.; Thermal decomposition rates for amorphous samples of penicillin G potassium, cephalothin sodium, cefamandole sodium, and cefamandole nafate were determined as a function of water content and temperature . Even when rigorously dry, amorphous cephalosporins were at least one order of magnitude less stable than the corresponding unsolvated crystalline form . Absorbed water generally increased both the number of decomposition products and the net decomposition rate . Reaction kinetics were usually apparent first order, but an anomalously high effective reaction order was observed in several systems . Nonlinear Arrhenius plots were observed, and a qualitative model based on molecular relaxation in glayses is proposed . Although decomposition rates at 25 degrees were small for dry samples, even slight decomposition produced visually detectable changes . Thus, the unsolvated crystalline form was noticeably more stable, even at 25 degrees. J Pharm Sci, 1977 Sep, 66(9), 1239 - 41 Smooth muscle relaxant properties and vasomotor actions of 2-amino-1-p-nitrophenylpropane-1,3-diol; Banerjee S et al.; Experiments with the guinea pig ileum, trachea, and vas deferens, the rat fundal strip, the rabbit jejunum and aortic strip, and the toad heart indicated that 2-amino-1-p-nitrophenylpropane-1,3-diol, the hydrolytic product of chloramphenicol, inhibited smooth muscles . Its action was direct and not through any mediators . After intravenous administration, the compound produced vasodepression followed by an overshooting rise of blood pressure . Vasodepression was not mediated by adrenergic, cholinergic, or histaminergic mechanisms . Hypertension was a sym