title: Antimicrobial activity and stability to beta-lactamase of BMY-28271, a new oral cephalosporin ester.
abstract: BMY-28271, the acetoxyethyl ester of BMY-28232, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3(Z) -propen-1-yl-3- cephem-4-carboxylic acid, is a new oral cephalosporin. BMY-28232 has a widely expanded spectrum with high activity against gram-positive and gram-negative bacteria. BMY-28232 is far more active than cefixime or cefteram against Staphylococcus aureus and Staphylococcus epidermidis. Against gram-negative bacteria, the activity of BMY-28232 was comparable to or somewhat weaker than that of cefixime or cefteram. BMY-28232 was a poor substrate for various beta-lactamases. Orally administered BMY-28271 had a good therapeutic effect on systemic infections with S. aureus and some gram-negative bacteria in mice. Oral BMY-28271 was efficacious against S. aureus Smith infection: the efficacy of BMY-28271 was 80 to 90 times higher than that of cefixime or cefteram.
authors.affiliation: Episome Institute, Gunma, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Matsui
authors.forename: M
authors.initials: M
authors.lastname: Hiraoka
authors.forename: M
authors.initials: M
authors.lastname: Inoue
authors.forename: S
authors.initials: S
authors.lastname: Mitsuhashi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D020682:Cefixime; D015281:Cefmenoxime / Q000031:analogs & derivatives / Q000494:pharmacology; D002439:Cefotaxime / Q000031:analogs & derivatives / Q000494:pharmacology; D002511:Cephalosporins / Q000008:administration & dosage / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D007700:Kinetics; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D013203:Staphylococcal Infections / Q000188:drug therapy*; D001618:beta-Lactamases
chemical_list: D002511:Cephalosporins; C060354:BMY 28271; C049493:cefteram; D020682:Cefixime; D001618:beta-Lactamases; D015281:Cefmenoxime; D002439:Cefotaxime