title: In vitro and in vivo evaluation of BMY 45243, a new 5-amino-naphthyridone derivative.
abstract: BMY 45243 is the first representative of 5-amino naphthyridone derivatives prepared following a new methodology developed by the authors. BMY 45243 is a highly lipophilic compound, very active in vitro and in vivo on S. aureus and was found to be as potent as ciprofloxacin on Gram-negative organisms with identical in vivo activity against Pseudomonas aeruginosa. Pharmacokinetics in mice showed better AUC and Cmax and longer t1/2 for BMY 45243 than for sparfloxacin and ciprofloxacin.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Lognes, France.
authors.forename: D
authors.initials: D
authors.lastname: Bouzard
authors.forename: P
authors.initials: P
authors.lastname: Di Cesare
authors.forename: P
authors.initials: P
authors.lastname: Hoffmann
authors.forename: J
authors.initials: J
authors.lastname: Fung-Tomc
authors.forename: R
authors.initials: R
authors.lastname: Kessler
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001424:Bacterial Infections / Q000188:drug therapy; D002939:Ciprofloxacin / Q000494:pharmacology; D005260:Female; D024841:Fluoroquinolones; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D015363:Quinolones / Q000494:pharmacology; D012995:Solubility
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D015363:Quinolones; C080343:BMY 45243; D002939:Ciprofloxacin; C061363:sparfloxacin