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新型氟化4-喹诺酮盐酸替马沙星(TA-167或A-62254)的体外活性

In vitro activity of temafloxacin hydrochloride (TA-167 or A-62254), a new fluorinated 4-quinolone.

作者信息

Nakanishi N, Inoue M, Inoue K, Yamaguchi T, Mitsuhashi S

机构信息

Episome Institute, Gunma, Japan.

出版信息

Chemotherapy. 1990;36(5):345-55. doi: 10.1159/000238787.

Abstract

The in vitro antibacterial activity of temafloxacin hydrochloride (TA-167 or A-62254) was evaluated against a wide variety of clinical isolates and compared with those of other fluoroquinolones. The potency (MIC90) of the compound against gram-positive aerobic bacteria was higher or comparable to those of ciprofloxacin, ofloxacin, and norfloxacin. Against most gram-negative enteric bacteria and Pseudomonas species, temafloxacin was less active than ciprofloxacin, but was generally as active as ofloxacin and norfloxacin, except against Proteus species and Morganella morganii. Against obligate anaerobes, it was more active than the reference quinolones. Temafloxacin was bactericidal for one strain each of Staphylococcus aureus. Escherichia coli, and Pseudomonas aeruginosa. The compound inhibited E. coli DNA gyrase activity at a low concentration.

摘要

评估了盐酸替马沙星(TA - 167或A - 62254)对多种临床分离株的体外抗菌活性,并与其他氟喹诺酮类药物进行了比较。该化合物对革兰氏阳性需氧菌的效力(MIC90)高于或与环丙沙星、氧氟沙星和诺氟沙星相当。对于大多数革兰氏阴性肠道细菌和假单胞菌属,替马沙星的活性低于环丙沙星,但一般与氧氟沙星和诺氟沙星活性相当,除了对变形杆菌属和摩根摩根菌。对于专性厌氧菌,它比参比喹诺酮类更具活性。替马沙星对金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌的各一个菌株具有杀菌作用。该化合物在低浓度下抑制大肠杆菌DNA回旋酶活性。

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