In vitro and in vivo activity of NY-198, a new difluorinated quinolone

Antimicrob Agents Chemother. 1987 Jun;31(6):854-9. doi: 10.1128/AAC.31.6.854.

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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Infective Agents / pharmacology*
  • Anti-Infective Agents / therapeutic use
  • Bacterial Infections / drug therapy
  • Fluoroquinolones*
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Norfloxacin / pharmacology
  • Norfloxacin / therapeutic use
  • Ofloxacin
  • Oxazines / pharmacology
  • Oxazines / therapeutic use
  • Pipemidic Acid / pharmacology
  • Pipemidic Acid / therapeutic use
  • Quinolines / pharmacology*
  • Quinolines / therapeutic use
  • Quinolones*

Substances

  • Anti-Infective Agents
  • Fluoroquinolones
  • Oxazines
  • Quinolines
  • Quinolones
  • Ofloxacin
  • lomefloxacin
  • Pipemidic Acid
  • Norfloxacin