In vitro antibacterial activity of KP-736, a new cephem antibiotic.
KP-736, a new cephen antibiotic with a broad antibacterial spectrum and potent antipseudomonal activity, was evaluated for in vitro antibacterial activity in comparison with ceftazidime, cefotaxime, and cefpirome. KP-736 was significantly more active than the test compounds against gram-negative bacteria, including the Pseudomonas group and ceftazidime-, cefotaxime-, or imipenem-resistant strains, but less active against gram-positive bacteria. KP-736 had very high affinities for penicillin-binding protein 3 (PBP 3) of Escherichia coli K-12 and PBP 1A and PBP 3 of Pseudomonas aerugiosa NCTC 10490 and showed potent bactericidal activities against these two strains. It was stable to hydrolysis by penicillinases and cephalosporinases but was slightly hydrolyzed by oxyiminocephalosporinases and type II penicillinase.
Maejima
T
T
Episome Institute, Gunma, Japan.
Inoue
M
M
Mitsuhashi
S
S
D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000494:pharmacology*; D001426:Bacterial Proteins; D002352:Carrier Proteins / Q000378:metabolism; D002439:Cefotaxime / Q000494:pharmacology; D002442:Ceftazidime / Q000494:pharmacology; D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D029968:Escherichia coli Proteins; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006602:Hexosyltransferases; D006868:Hydrolysis; D008826:Microbial Sensitivity Tests; D002267:Muramoylpentapeptide Carboxypeptidase / Q000378:metabolism; D046915:Penicillin-Binding Proteins; D046928:Peptidoglycan Glycosyltransferase; D010458:Peptidyl Transferases; D013997:Time Factors; D001618:beta-Lactamases / Q000378:metabolism
D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D002352:Carrier Proteins; D002511:Cephalosporins; D029968:Escherichia coli Proteins; C478704:FtsI protein, E coli; D046915:Penicillin-Binding Proteins; C068216:KP 736; D002442:Ceftazidime; D010458:Peptidyl Transferases; D006602:Hexosyltransferases; D046928:Peptidoglycan Glycosyltransferase; D002267:Muramoylpentapeptide Carboxypeptidase; D001618:beta-Lactamases; D002439:Cefotaxime