Ito T, Otsuki M, Nishino T
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Antimicrob Agents Chemother. 1992 Aug;36(8):1708-14. doi: 10.1128/AAC.36.8.1708.
The in vitro activity of Q-35, an 8-methoxy fluoroquinolone, was compared with those of ofloxacin, ciprofloxacin, tosufloxacin, lomefloxacin, and sparfloxacin. The MICs of Q-35 for 90% of strains tested (MIC90s) of Staphylococcus aureus, methicillin-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Streptococcus pyogenes were 0.2, 6.25, 0.2, 0.39, and 0.39 micrograms/ml, respectively. The activity of Q-35 was 4- to 16-fold greater than those of ofloxacin, ciprofloxacin and lomefloxacin but equal to those of tosufloxacin and sparfloxacin against these organisms. For 82 ciprofloxacin-resistant staphylococci (MIC90 = 100 micrograms/ml), Q-35 was the most active of the new quinolones tested (MIC90 = 6.25 micrograms/ml). The MIC90s of Q-35 against Escherichia coli, Enterobacter aerogenes, and Pseudomonas aeruginosa were 0.2, 0.78, and 12.5 micrograms/ml, respectively, and Q-35 was 2- to 16-fold less active than the other quinolones tested. Q-35 showed potent bactericidal activity and inhibited the supercoiling activity of DNA gyrase of S. aureus, E. coli, and P. aeruginosa.
将8-甲氧基氟喹诺酮Q-35的体外活性与氧氟沙星、环丙沙星、妥舒沙星、洛美沙星和司帕沙星进行了比较。Q-35对金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌、肺炎链球菌和化脓性链球菌90%受试菌株(MIC90)的最低抑菌浓度(MIC)分别为0.2、6.25、0.2、0.39和0.39微克/毫升。Q-35对这些菌的活性比对氧氟沙星、环丙沙星和洛美沙星高4至16倍,但与妥舒沙星和司帕沙星相当。对于82株耐环丙沙星葡萄球菌(MIC90 = 100微克/毫升),Q-35是受试新型喹诺酮类药物中活性最高的(MIC90 = 6.25微克/毫升)。Q-35对大肠杆菌、产气肠杆菌和铜绿假单胞菌的MIC90分别为0.2、0.78和12.5微克/毫升,其活性比其他受试喹诺酮类药物低2至16倍。Q-35表现出强大的杀菌活性,并抑制金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌DNA促旋酶的超螺旋活性。