Masuda N, Takahashi Y, Otsuki M, Ibuki E, Miyoshi H, Nishino T
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Antimicrob Agents Chemother. 1996 May;40(5):1201-7. doi: 10.1128/AAC.40.5.1201.
The in vitro and in vivo activities of CS-940, a new 6-fluoro-8-difluoromethoxy quinolone, were compared with those of ciprofloxacin, tosufloxacin, sparfloxacin, and levofloxacin. The in vitro activity of CS-940 against gram-positive bacteria was nearly equal to or greater than those of the other quinolones tested. In particular, CS-940 was two to eight times more active against methicillin-resistant Staphylococcus aureus than the other quinolones, at the MIC at which 90% of the clinical isolates are inhibited. Against gram-negative bacteria, the activity of CS-940 was comparable to or greater than those of tosufloxacin, sparfloxacin, and levofloxacin, while it was lower than that of ciprofloxacin. The activity of CS-940 was largely unaffected by medium, inoculum size, or the addition of horse serum, but it was decreased under acidic conditions, as was also seen with the other quinolones tested. CS-940 showed potent bactericidal activity against S. aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. In oral treatment of mouse systemic infections caused by S. aureus, Streptococcus pneumoniae, Streptococcus pyogenes, E. coli, K. pneumoniae, Serratia marcescens, and P. aeruginosa, CS-940 was more effective than ciprofloxacin, sparfloxacin, and levofloxacin against all strains tested. Against experimental pneumonia with K. pneumoniae in mice, CS-940 was the most effective of all the quinolones tested. These results suggest that CS-940 may be effective in the therapy of various bacterial infections.
将新型6-氟-8-二氟甲氧基喹诺酮CS-940的体外和体内活性与环丙沙星、妥舒沙星、司帕沙星和左氧氟沙星进行了比较。CS-940对革兰氏阳性菌的体外活性几乎等于或高于所测试的其他喹诺酮类药物。特别是，在抑制90%临床分离株的最低抑菌浓度下，CS-940对耐甲氧西林金黄色葡萄球菌的活性比其他喹诺酮类药物高2至8倍。对革兰氏阴性菌，CS-940的活性与妥舒沙星、司帕沙星和左氧氟沙星相当或更高，而低于环丙沙星。CS-940的活性在很大程度上不受培养基、接种量或添加马血清的影响，但在酸性条件下会降低，其他所测试的喹诺酮类药物也有此现象。CS-940对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌显示出强大的杀菌活性。在口服治疗由金黄色葡萄球菌、肺炎链球菌、化脓性链球菌、大肠杆菌、肺炎克雷伯菌、粘质沙雷氏菌和铜绿假单胞菌引起的小鼠全身感染时，CS-940对所有测试菌株的疗效均优于环丙沙星、司帕沙星和左氧氟沙星。在小鼠肺炎克雷伯菌所致的实验性肺炎中，CS-940是所有测试喹诺酮类药物中最有效的。这些结果表明，CS-940可能对各种细菌感染的治疗有效。
