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新型6-氟-8-甲氧基喹诺酮AM-1155的体外抗菌活性

In vitro antibacterial activity of AM-1155, a novel 6-fluoro-8-methoxy quinolone.

作者信息

Wakabayashi E, Mitsuhashi S

机构信息

Episome Institute, Gunma, Japan.

出版信息

Antimicrob Agents Chemother. 1994 Mar;38(3):594-601. doi: 10.1128/AAC.38.3.594.

Abstract

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.

摘要

将AM - 1155对多种临床分离株的体外抗菌活性与其他氟喹诺酮类药物进行了比较。AM - 1155对90%的受试金黄色葡萄球菌、肺炎链球菌和粪肠球菌分离株的最低抑菌浓度(MIC)分别为0.10、0.39和0.78微克/毫升。AM - 1155对革兰氏阳性菌和厌氧菌的抗菌活性与司帕沙星和妥舒沙星相当。AM - 1155在浓度为0.39微克/毫升时可抑制90%的大多数肠杆菌科菌种。AM - 1155对革兰氏阴性菌的活性一般与司帕沙星相当。AM - 1155对耐甲氧西林和耐喹诺酮的金黄色葡萄球菌表现出中等活性。AM - 1155在MIC时表现出杀菌活性。对于金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌,对四倍AM - 1155 MIC耐药的自发突变体出现频率<1×10⁻⁹。AM - 1155强烈抑制从大肠杆菌和金黄色葡萄球菌中纯化的DNA旋转酶的超螺旋活性。

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