title: In vitro and in vivo activity of NY-198, a new difluorinated quinolone.
abstract: NY-198 [1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3- quinolinecarboxylic acid hydrochloride] is a new difluorinated quinolone characterized by the presence of a C-methyl group at the 3 position of the piperazine moiety. It has a broad antibacterial spectrum. The in vitro antibacterial activity of NY-198 was almost the same as those of ofloxacin and norfloxacin, but far exceeded that of pipemidic acid. NY-198 was more active than norfloxacin against Pseudomonas maltophilia, Acinetobacter calcoaceticus, and anaerobic microorganisms. Cross resistance was not observed between NY-198 and various antibiotics including methicillin, gentamicin, and ampicillin. NY-198 had bactericidal activity at the MIC or slightly higher than the MIC. It showed excellent antibacterial activity against various systemic infections in mice. After oral administration, NY-198 was two times more active than or as active as ofloxacin and two to four times more active than norfloxacin.
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001424:Bacterial Infections / Q000188:drug therapy; D024841:Fluoroquinolones; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000494:pharmacology / Q000627:therapeutic use; D015242:Ofloxacin; D010078:Oxazines / Q000494:pharmacology / Q000627:therapeutic use; D010876:Pipemidic Acid / Q000494:pharmacology / Q000627:therapeutic use; D011804:Quinolines / Q000494:pharmacology* / Q000627:therapeutic use; D015363:Quinolones
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D010078:Oxazines; D011804:Quinolines; D015363:Quinolones; D015242:Ofloxacin; C053091:lomefloxacin; D010876:Pipemidic Acid; D009643:Norfloxacin