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环丙沙星与其他五种喹啉衍生物对革兰氏阴性菌分离株的体外活性比较

Comparative in vitro activity of ciprofloxacin and five other quinoline derivatives against gram-negative isolates.

作者信息

Galante D, Pennucci C, Esposito S, Barba D

出版信息

Drugs Exp Clin Res. 1985;11(5):331-4.

PMID:2941260
Abstract

A total of 375 Gram-negative bacterial strains were isolated from midstream urine specimens of the same number of patients affected by urinary tract infections. All bacteria were identified by standard bacteriological methods and their susceptibility to six quinoline derivatives (ciprofloxacin, cinoxacin, norfloxacin, oxolinic acid, pipemidic acid, nalidixic acid) was studied by determining the MICs and MBCs for each compound using a miniaturized dilution broth method in microtitre plates and twofold dilutions of each drug from 256 to 0.12 mcg/ml. Ciprofloxacin, a new quinoline carboxylic acid compound structurally related to nalidixic acid, showed a much higher antibacterial activity against all bacterial strains under examination, including Pseudomonas, than the other compounds, except for norfloxacin. The MIC90 and MBC90 of ciprofloxacin never exceeded 1 mcg/ml with any of the bacterial species; and MBC/MIC ratios were very low, which represents an important clinical advantage. Only norfloxacin showed comparable effectiveness. No bacterial strain showed resistance to the drug and the MIC90 and MBC90 never exceeded 8 mcg/ml.

摘要

从相同数量的尿路感染患者的中段尿标本中总共分离出375株革兰氏阴性菌。所有细菌均采用标准细菌学方法进行鉴定,并通过微量滴定板中的小型化稀释肉汤法以及将每种药物从256至0.12 mcg/ml进行两倍稀释来测定每种化合物的最低抑菌浓度(MIC)和最低杀菌浓度(MBC),研究它们对六种喹啉衍生物(环丙沙星、西诺沙星、诺氟沙星、恶喹酸、吡哌酸、萘啶酸)的敏感性。环丙沙星是一种结构上与萘啶酸相关的新型喹啉羧酸化合物,除诺氟沙星外,它对包括假单胞菌在内的所有受试菌株显示出比其他化合物高得多的抗菌活性。环丙沙星对任何细菌种类的MIC90和MBC90从未超过1 mcg/ml;且MBC/MIC比值非常低,这代表着重要的临床优势。只有诺氟沙星显示出相当的有效性。没有菌株对该药物耐药,其MIC90和MBC90从未超过8 mcg/ml。

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