In vitro antibacterial activity of AM-1155, a novel 6-fluoro-8-methoxy quinolone.
The in vitro antibacterial activity of AM-1155 against a wide variety of clinical isolates was compared with those of other fluoroquinolones. The MICs of AM-1155 for 90% of Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis isolates tested were 0.10, 0.39, and 0.78 microgram/ml, respectively. The antibacterial activity of AM-1155 against gram-positive bacteria and anaerobes was comparable to those of sparfloxacin and tosufloxacin. AM-1155 inhibited 90% of most species of the family Enterobacteriaceae at a concentration of 0.39 microgram/ml. AM-1155 generally had activity comparable to that of sparfloxacin against gram-negative bacteria. AM-1155 showed moderate activity against methicillin- and quinolone-resistant S. aureus. AM-1155 demonstrated bactericidal activity at the MIC. The frequency of occurrence of spontaneous mutants resistant to four times the MIC of AM-1155 was < 1 x 10(9) for S. aureus, Escherichia coli, and Pseudomonas aeruginosa. AM-1155 strongly inhibited the supercoiling activities of DNA gyrases purified from E. coli and S. aureus.
Wakabayashi
E
E
Episome Institute, Gunma, Japan.
Mitsuhashi
S
S
D000890:Anti-Infective Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000235:genetics; D001424:Bacterial Infections / Q000382:microbiology; D004352:Drug Resistance, Microbial / Q000235:genetics; D024841:Fluoroquinolones; D000077734:Gatifloxacin; D006801:Humans; D007564:Japan; D008826:Microbial Sensitivity Tests; D009154:Mutation; D010879:Piperazines / Q000494:pharmacology*; D015363:Quinolones / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D010879:Piperazines; D015363:Quinolones; D059005:Topoisomerase II Inhibitors; D000077734:Gatifloxacin