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新型氟喹诺酮类药物T-3262的体外和体内抗菌活性

In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone.

作者信息

Fujimaki K, Noumi T, Saikawa I, Inoue M, Mitsuhashi S

机构信息

Episome Institute, Gunma, Japan.

出版信息

Antimicrob Agents Chemother. 1988 Jun;32(6):827-33. doi: 10.1128/AAC.32.6.827.

Abstract

T-3262, a new fluoroquinolone, showed a broad spectrum of activity against gram-positive and gram-negative bacteria. T-3262 had most potent activity against gram-positive cocci, such as Staphylococcus, Streptococcus, and Enterococcus spp. The MICs of T-3262 for 90% of strains tested were between 0.05 and 1.56 micrograms/ml. Against members of the family Enterobacteriaceae and Pseudomonas aeruginosa, the activities of T-3262 were almost equal to those of ciprofloxacin. Obligate anaerobes were also susceptible to T-3262. T-3262 was bactericidal for one strain each of Staphylococcus aureus, Escherichia coli, and P. aeruginosa at concentrations near its MIC; and fluoroquinolones, including T-3262, inhibited DNA gyrase activity at low concentrations. The 50% effective dose of T-3262 after oral administration against systemic infections with S. aureus in mice was about 6 times lower than that of ofloxacin and about 20 times lower than that of norfloxacin.

摘要

新型氟喹诺酮类药物T - 3262对革兰氏阳性菌和革兰氏阴性菌均显示出广谱抗菌活性。T - 3262对革兰氏阳性球菌,如葡萄球菌、链球菌和肠球菌属具有最强的活性。T - 3262对90%受试菌株的最低抑菌浓度(MIC)在0.05至1.56微克/毫升之间。对于肠杆菌科成员和铜绿假单胞菌,T - 3262的活性几乎与环丙沙星相当。专性厌氧菌也对T - 3262敏感。T - 3262在接近其MIC的浓度下,对金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌各一株具有杀菌作用;包括T - 3262在内的氟喹诺酮类药物在低浓度下可抑制DNA旋转酶活性。小鼠口服T - 3262后,针对金黄色葡萄球菌全身感染的50%有效剂量比氧氟沙星低约6倍,比诺氟沙星低约20倍。

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