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136821. In vitro antibacterial activities of PD 131628, a new 1,8-naphthyridine anti-infective agent. Full Text available with Trip Pro

In vitro antibacterial activities of PD 131628, a new 1,8-naphthyridine anti-infective agent. PD 131628 is a new aminopyrrolidine-substituted fluorocyclopropyl naphthyridine quinolone which possesses high in vitro activity against a wide spectrum of bacterial species. The MICs for greater than or equal to 90% of strains were 0.125 to 0.25 microgram/ml for staphylococci, Streptococcus pyogenes, and S. pneumoniae; 0.5 micrograms/ml for S. agalactiae and Enterococcus faecalis; 0.125 micrograms/ml

1991 Antimicrobial Agents and Chemotherapy

136822. Comparative in vitro antibacterial activity of sparfloxacin (AT-4140; RP 64206), a new quinolone. Full Text available with Trip Pro

Comparative in vitro antibacterial activity of sparfloxacin (AT-4140; RP 64206), a new quinolone. The in vitro activity of sparfloxacin (AT-4140; RP 64206), a new fluoroquinolone, was compared with those of 10 other agents against 1,222 clinical isolates. Sparfloxacin and ciprofloxacin were the most active quinolones against members of the family Enterobacteriaceae and nonfermenting gram-negative bacilli; sparfloxacin had superior activity against gram-positive cocci in comparison (...) with the activities of ciprofloxacin and the other quinolones tested (norfloxacin, lomefloxacin, and pefloxacin). Among the inhibited strains, several were resistant to the tested beta-lactam antibiotics or to aminoglycosides. The activity of sparfloxacin was not influenced by the medium that was used; lowering of the pH to 5 had a marked effect on the MICs for two strains each of Enterobacter cloacae and Pseudomonas aeruginosa and one strain each of Escherichia coli and Staphylococcus aureus; the MBC

1991 Antimicrobial Agents and Chemotherapy

136823. Intrinsic and unusual resistance to macrolide, lincosamide, and streptogramin antibiotics in bacteria. Full Text available with Trip Pro

Intrinsic and unusual resistance to macrolide, lincosamide, and streptogramin antibiotics in bacteria. 1929281 1991 11 04 2018 11 13 0066-4804 35 7 1991 Jul Antimicrobial agents and chemotherapy Antimicrob. Agents Chemother. Intrinsic and unusual resistance to macrolide, lincosamide, and streptogramin antibiotics in bacteria. 1273-6 Leclercq R R Service de Bactériologie-Virologie-Hygiène, Hôpital Henri Mondor, Université Paris XII, Créteil, France. Courvalin P P eng Journal Article Review (...) Microbiol (Paris). 1981 Nov-Dec;132 B(3):419-27 7036825 J Antibiot (Tokyo). 1984 Dec;37(12):1692-6 6396291 Gene. 1985;35(3):271-8 3899861 J Antimicrob Chemother. 1985 Jul;16 Suppl A:137-49 3932300 Antimicrob Agents Chemother. 1986 Mar;29(3):515-8 3521489 Nucleic Acids Res. 1986 Jun 25;14(12):4987-99 3523438 Antimicrob Agents Chemother. 1986 Nov;30(5):653-8 3800341 Antimicrob Agents Chemother. 1986 Nov;30(5):694-700 3541783 Antimicrob Agents Chemother. 1987 Mar;31(3):404-9 3579257 Antimicrob Agents

1991 Antimicrobial Agents and Chemotherapy

136824. Mechanisms of interaction among subinhibitory concentrations of antibiotics, human polymorphonuclear neutrophils, and gram-negative bacilli. Full Text available with Trip Pro

Mechanisms of interaction among subinhibitory concentrations of antibiotics, human polymorphonuclear neutrophils, and gram-negative bacilli. Our hypothesis was that pretreatment of bacteria with subinhibitory concentrations (sub-MICs) of antibiotics enhances the susceptibility of the organisms to killing by human polymorphonuclear neutrophils (PMNs). Our purpose was to study a variety of drugs with different mechanisms of action and to determine whether the mechanism and locus of action altered (...) the sub-MIC effect. The following outcome measures were used: ingestion and killing of bacteria by PMNs, bacterial killing in the absence of phagosome formation, and binding requirements of the bacteria to PMNs. The antibiotics used were representative of a variety of classes, including beta-lactams (piperacillin and imipenem) and quinolones (ciprofloxacin). Bacterial uptake and killing were measured by using standard techniques, and results were analyzed by using the analysis-of-variance technique

1991 Antimicrobial Agents and Chemotherapy

136825. Bacterial resistance to macrolide, lincosamide, and streptogramin antibiotics by target modification. Full Text available with Trip Pro

Bacterial resistance to macrolide, lincosamide, and streptogramin antibiotics by target modification. 1929280 1991 11 04 2018 11 13 0066-4804 35 7 1991 Jul Antimicrobial agents and chemotherapy Antimicrob. Agents Chemother. Bacterial resistance to macrolide, lincosamide, and streptogramin antibiotics by target modification. 1267-72 Leclercq R R Service de Bactériologie-Virologie-Hygiène, Hôpital Henri Mondor, Université Paris XII, Créteil, France. Courvalin P P eng Journal Article Review United

1991 Antimicrobial Agents and Chemotherapy

136826. Cardiovascular and autonomic pharmacology of the macrolide antibiotic LY281389 in anesthetized beagles and in isolated smooth and cardiac muscles. Full Text available with Trip Pro

of greater than or equal to 200 micrograms/kg of body weight. LY281389 also produced slight increases in mean arterial pressure and shortening of the P-R interval of the electrocardiogram. In summary, LY281389 possesses nonselective receptor antagonist activity in vitro and produces cardiovascular stimulation in anesthetized dogs. These results indicate that, in addition to potent antimicrobial activity, the macrolide antibiotic LY281389 may exert unexpected actions on cardiovascular function. (...) Cardiovascular and autonomic pharmacology of the macrolide antibiotic LY281389 in anesthetized beagles and in isolated smooth and cardiac muscles. As part of the preclinical safety evaluation process, an investigational macrolide antibiotic, LY281389, was examined for autonomic activity in isolated smooth and cardiac muscle preparations and for cardiovascular effects by intravenous infusion in anesthetized beagles. Concentration-dependent antagonism of acetylcholine and angiotensin I (guinea

1991 Antimicrobial Agents and Chemotherapy

136827. Renal dehydropeptidase-I stability of LJC 10,627, a new carbapenem antibiotic. Full Text available with Trip Pro

Renal dehydropeptidase-I stability of LJC 10,627, a new carbapenem antibiotic. LJC 10,627 is a new parenteral carbapenem antibiotic. LJC 10,627 stability against human renal dehydropeptidase-I was compared with that of imipenem. Hydrolysis of this compound was not detectable by spectrophotometrical assay. Even after a 2-h incubation of antibiotics with this enzyme at 30 degrees C, the concentration of LJC 10,627 remained at 92.3% of the initial concentration, whereas imipenem completely

1992 Antimicrobial Agents and Chemotherapy

136828. Cloning of the complete biosynthetic gene cluster for an aminonucleoside antibiotic, puromycin, and its regulated expression in heterologous hosts. Full Text available with Trip Pro

Cloning of the complete biosynthetic gene cluster for an aminonucleoside antibiotic, puromycin, and its regulated expression in heterologous hosts. Puromycin, produced by Streptomyces alboniger, is a member of the large group of aminonucleoside antibiotics. The genes pac and dmpM, encoding a puromycin N-acetyl transferase and an O-demethyl puromycin O-methyltransferase, respectively, are tightly linked in the DNA of S. alboniger. The entire set of genes encoding the puromycin biosynthesis

1992 The EMBO journal

136829. Role of antibiotic production by Erwinia herbicola Eh252 in biological control of Erwinia amylovora. Full Text available with Trip Pro

Role of antibiotic production by Erwinia herbicola Eh252 in biological control of Erwinia amylovora. Erwinia herbicola Eh252 is a nonpathogenic epiphytic bacterium that reduces fire blight incidence when sprayed onto apple blossoms before inoculation with Erwinia amylovora, the causal agent of fire blight. Eh252 was found to produce on minimal medium an antibiotic that inhibited the growth of E. amylovora. This antibiotic was inactivated by histidine but not by Fe(II), was sensitive (...) to proteolytic enzymes, and showed a narrow host range of activity. To determine the role of this antibiotic in the control of fire blight, two prototrophic Tn5-induced mutants, 10:12 and 17:12, that had lost their ability to inhibit E. amylovora on plates (Ant- mutants) were compared with the wild-type strain for their ability to suppress fire blight in immature pear fruits. The two mutants had single Tn5 insertions in the chromosome; although they grew in immature pear fruits at a rate similar

1992 Journal of bacteriology

136830. Inhibitory potency of quinolone antibacterial agents against cytochrome P450IA2 activity in vivo and in vitro. Full Text available with Trip Pro

Inhibitory potency of quinolone antibacterial agents against cytochrome P450IA2 activity in vivo and in vitro. Inhibition of cytochrome P450IA2 activity is an important adverse effect of quinolone antibacterial agents. It results in a prolonged half-life for some drugs that are coadministered with quinolones, such as theophylline. The objective of the study described here was to define the parameters for quantifying the inhibitory potencies of quinolones against cytochrome P450IA2 in vivo

1992 Antimicrobial Agents and Chemotherapy

136831. Susceptibility of Pseudomonas species to the novel antibiotics mureidomycins. Full Text available with Trip Pro

Susceptibility of Pseudomonas species to the novel antibiotics mureidomycins. Strains of Pseudomonas aeruginosa, including imipenem- or ofloxacin-resistant clinical isolates, and some other species in the genus Pseudomonas were inhibited by novel antibiotics of the mureidomycin (MRD) group. On the other hand, almost all other gram-positive and gram-negative bacteria were resistant to MRDs, though the antibiotics potently inhibited the in vitro peptidoglycan synthesis of Escherichia coli and P

1992 Antimicrobial Agents and Chemotherapy

136832. In vivo antibiotic synergism: contribution of animal models. Full Text available with Trip Pro

In vivo antibiotic synergism: contribution of animal models. 1510412 1992 09 22 2018 11 13 0066-4804 36 5 1992 May Antimicrobial agents and chemotherapy Antimicrob. Agents Chemother. In vivo antibiotic synergism: contribution of animal models. 907-12 Fantin B B Service de Médecine Interne, Hôpital Bichat, Paris, France. Carbon C C eng Journal Article Review United States Antimicrob Agents Chemother 0315061 0066-4804 0 Anti-Bacterial Agents IM Animals Anti-Bacterial Agents Bacterial Infections

1992 Antimicrobial Agents and Chemotherapy

136833. Is antibiotic penetration compromised in the ischaemic tissues of patients undergoing amputation? Full Text available with Trip Pro

Is antibiotic penetration compromised in the ischaemic tissues of patients undergoing amputation? Antibiotic prophylaxis is indicated for patients undergoing amputation for severe ischaemia or gangrene. However, the adequacy of tissue levels of antibiotics in ischaemic tissue is not known. In this study the serum and tissue antibiotic levels were measured after intravenous administration of metronidazole (15 mg/kg body weight) and cephradine (20 mg/kg body weight). In 11 patients, venous

1992 Annals of the Royal College of Surgeons of England

136834. Roles of peripheral leukocytes and tissue macrophages in antibacterial resistance induced by free or liposome-encapsulated muramyl tripeptide phosphatidylethanolamide. Full Text available with Trip Pro

Roles of peripheral leukocytes and tissue macrophages in antibacterial resistance induced by free or liposome-encapsulated muramyl tripeptide phosphatidylethanolamide. Administration of free muramyl tripeptide phosphatidylethanolamide (MTPPE) or liposome-encapsulated MTPPE (LE-MTPPE) in a twofold-lower dose at 24 h before bacterial inoculation resulted in clearance of intravenously inoculated Klebsiella pneumoniae by tissue macrophages, whereas in control mice, bacteria were not effectively (...) cleared from the blood. In addition, MTPPE and LE-MTPPE led to increased numbers of leukocytes in the blood, which could compensate for the leukopenia in mice resulting from infection with K. pneumoniae. In an attempt to elucidate the relative contributions of the activation of tissue macrophages and the recruitment of leukocytes to the antibacterial resistance induced by MTPPE and LE-MTPPE, mice were infected intraperitoneally with K. pneumoniae. In these MTPPE- and LE-MTPPE treated mice

1992 Infection and immunity

136835. Comparison of the effects of the new azalide antibiotic, azithromycin, and erythromycin estolate on rat liver cytochrome P-450. Full Text available with Trip Pro

Comparison of the effects of the new azalide antibiotic, azithromycin, and erythromycin estolate on rat liver cytochrome P-450. Erythromycin and some other macrolide antibiotics can first induce a cytochrome P-450 isozyme similar to the one induced in rats by pregnenolone-16 alpha-carbonitrile and then inhibit it by forming a stable cytochrome P-450-metabolite complex. The purpose of this study was to compare azithromycin, a novel 15-membered ring azalide, and erythromycin estolate

1991 Antimicrobial Agents and Chemotherapy

136836. Use of slime dispersants to promote antibiotic penetration through the extracellular polysaccharide of mucoid Pseudomonas aeruginosa. Full Text available with Trip Pro

Use of slime dispersants to promote antibiotic penetration through the extracellular polysaccharide of mucoid Pseudomonas aeruginosa. Agents with the potential to reduce Pseudomonas aeruginosa alginate viscosity (slime dispersants) were shown to promote the diffusion of antipseudomonal antibiotics through alginate but were more effective in facilitating the diffusion of gentamicin than that of ceftazidime. EDTA increased the diffusion rates of these antibiotics by factors of 4.0 and 1.5

1991 Antimicrobial Agents and Chemotherapy

136837. Analysis of murein and murein precursors during antibiotic-induced lysis of Escherichia coli. Full Text available with Trip Pro

Analysis of murein and murein precursors during antibiotic-induced lysis of Escherichia coli. Lysis of Escherichia coli induced by either D-cycloserine, moenomycin, or penicillin G was monitored by studying murein metabolism. The levels of the soluble murein precursor UDP-N-acetylmuramyl-L-alanyl-D-glutamyl-m-diaminopimelyl-D-alanyl- D-alanine (UDP-MurNAc-pentapeptide) and the carrier-linked MurNAc-(pentapeptide)-pyrophosphoryl-undecaprenol as well as N-acetylglucosamine-beta-1,4-MurNAc (...) strands decreased. When the glycan strands were fractionated according to length, a dramatic increase in the amount of single disaccharide units was observed not only in the presence of penicillin but also in the presence of moenomycin. This result is explained by the action of an exo-muramidase, such as the lytic transglycosylases present in E. coli. It is proposed that antibiotic-induced bacteriolysis is the result of a zipperlike splitting of the murein net by exo-muramidases locally restricted

1991 Journal of bacteriology

136838. Effect of protein binding in serum on therapeutic efficacy of cephem antibiotics. Full Text available with Trip Pro

Effect of protein binding in serum on therapeutic efficacy of cephem antibiotics. The effect of protein binding in serum of eight cephem antibiotics (ceftazidime, ceftizoxime, cefotiam, cefmetazole, cefpiramide, cefazolin, cefuzonam, ceftriaxone) on their therapeutic efficacies was examined in mice with experimentally induced intraperitoneal infections or pneumonia. The relationship among therapeutic activity, in vitro antibacterial activity, total or free (unbound) levels in serum (...) , and homogenized whole lung levels was investigated. In the intraperitoneal infection caused by Staphylococcus aureus or Klebsiella pneumoniae, the 50% effective doses (ED50s) of the cephem antibiotics correlated with the area under the concentration-time curve (AUC) values of free levels in serum and the MICs but not with those of total levels in serum. A linear relationship was seen between 1/ED50 values and AUC of free levels in serum/MIC values. On the other hand, in mice with pneumonia caused by K

1992 Antimicrobial Agents and Chemotherapy

136839. Induction of calf thymus topoisomerase II-mediated DNA breakage by the antibacterial isothiazoloquinolones A-65281 and A-65282. Full Text available with Trip Pro

Induction of calf thymus topoisomerase II-mediated DNA breakage by the antibacterial isothiazoloquinolones A-65281 and A-65282. A number of quinolones and related antibacterial compounds were screened for activity against calf thymus topoisomerase II by using the P4 unknotting and DNA breakage assays. Several compounds from different structural classes which inhibited DNA unknotting with 50% inhibitory concentrations ranging from 8 to 25 micrograms/ml were identified. Two experimental (...) both bacterial and eukaryotic type II topoisomerases. The implications of these data for the selectivity of topoisomerase-directed compounds and the potential toxicity of such compounds developed as antibacterial agents are discussed.

1992 Antimicrobial Agents and Chemotherapy

136840. In vitro and in vivo activities of SCE-2787, a new parenteral cephalosporin with a broad antibacterial spectrum. Full Text available with Trip Pro

In vitro and in vivo activities of SCE-2787, a new parenteral cephalosporin with a broad antibacterial spectrum. SCE-2787, a new cephalosporin having a condensed azolium moiety in the 3 position and an aminothiadiazolyl group in the 7 beta side chain, was evaluated for its in vitro and in vivo activities in comparison with those of ceftazidime, flomoxef, cefpirome, and E1040. Against methicillin-susceptible strains of Staphylococcus aureus and Staphylococcus epidermidis, SCE-2787 was more (...) of the antibiotics tested. The activities of SCE-2787 against Streptococcus species, most members of the family Enterobacteriaceae, and Haemophilus influenzae exceeded those of ceftazidime and flomoxef and were comparable to those of cefpirome. Furthermore, MIC90s of SCE-2787 were significantly lower than those of ceftazidime for ceftazidime-resistant isolates of Citrobacter freundii and Enterobacter cloacae. SCE-2787 was resistant to hydrolysis by various types of beta-lactamases, including the Bush group 1

1992 Antimicrobial Agents and Chemotherapy

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