In-vitro and in-vivo activities of T-3262, a new pyridone carboxylic acid.
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.
Takahata
M
M
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Otsuki
M
M
Nishino
T
T
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology*; D001420:Bacteria, Aerobic / Q000187:drug effects*; D001421:Bacteria, Anaerobic / Q000187:drug effects*; D004352:Drug Resistance, Microbial; D024841:Fluoroquinolones; D006863:Hydrogen-Ion Concentration; D008274:Magnesium / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines; D011014:Pneumonia / Q000188:drug therapy
D042462:4-Quinolones; D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; C055185:tosufloxacin; D008274:Magnesium