In vitro evaluation of U63196-E (AC-1370): antimicrobial activity, beta-lactamase stability, and beta-lactamase inhibition.
Upjohn compound U63196 -E (formerly AC-1370) is a new semisynthetic cephalosporin with a broad spectrum of antimicrobial activity that includes Pseudomonas aeruginosa (minimum inhibitory concentration, 8.0 micrograms/ml), nearly all members of the Enterobacteriaceae, and most gram-positive cocci except enterococci and staphylococci resistant to to methicillin. The compound was stable to most commonly isolated beta-lactamases, especially TEM-1, TEM-2, and P-99; the highest rates of hydrolysis of U63196 -E were by PSE enzymes (23.4-92.5% of the relative hydrolysis rate of cephaloridine). Compared to eight other beta-lactams, U63196 -E was a poor inhibitor of beta-lactamases.
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D002511:Cephalosporins / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004352:Drug Resistance, Microbial; D004755:Enterobacteriaceae / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D065093:beta-Lactamase Inhibitors; C038845:cefpimizole; D001618:beta-Lactamases