In vitro and in vivo evaluation of BMY 45243, a new 5-amino-naphthyridone derivative.
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.
Bouzard
D
D
Bristol-Myers Squibb Pharmaceutical Research Institute, Lognes, France.
Di Cesare
P
P
Hoffmann
P
P
Fung-Tomc
J
J
Kessler
R
R
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
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D015363:Quinolones; C080343:BMY 45243; D002939:Ciprofloxacin; C061363:sparfloxacin