In-vitro and in-vivo activities of T-3262, a new pyridone carboxylic acid

J Antimicrob Chemother. 1988 Aug;22(2):143-54. doi: 10.1093/jac/22.2.143.

Abstract

T-3262[p-toluenesulfonic acid salt of dl-7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylic acid monohydrate] is a new pyridone carboxylic acid with a broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria. The activity of T-3262 against most Enterobacteriaceae was comparable with that of ciprofloxacin except Proteus spp. and Providencia rettgeri and exceeded that of ofloxacin and norfloxacin. The activity of T-3262 against Pseudomonas aeruginosa was comparable with that of ciprofloxacin, and T-3262 was more active than the other new quinolones against Acinetobacter calcoaceticus, Branhamella catarrhalis and Haemophilus influenzae, and also against staphylococci, streptococci, and Bacteroides fragilis. The protective effects of a single oral dose of T-3262 on systemic infection in mice were greater than norfloxacin. T-3262 was as effective as ofloxacin and ciprofloxacin against systemic infections in an animal model with Escherichia coli and Klebsiella pneumoniae, and more active against Ps. aeruginosa infections. T-3262 showed excellent activity against staphylococcal and streptococcal infections.

Publication types

  • Comparative Study

MeSH terms

  • 4-Quinolones
  • Animals
  • Anti-Infective Agents / pharmacology*
  • Bacteria, Aerobic / drug effects*
  • Bacteria, Anaerobic / drug effects*
  • Drug Resistance, Microbial
  • Fluoroquinolones*
  • Hydrogen-Ion Concentration
  • Magnesium / pharmacology
  • Male
  • Mice
  • Mice, Inbred ICR
  • Microbial Sensitivity Tests
  • Naphthyridines*
  • Pneumonia / drug therapy

Substances

  • 4-Quinolones
  • Anti-Infective Agents
  • Fluoroquinolones
  • Naphthyridines
  • tosufloxacin
  • Magnesium