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首页> 外文期刊>Anti-infective agents in medicinal chemistry >Laboratorio di Chimica Bioorganica, Dipartimento di Fisica, Universita di Trento, via Sommarive 14, I-38050 Povo-Trento, Italy
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Laboratorio di Chimica Bioorganica, Dipartimento di Fisica, Universita di Trento, via Sommarive 14, I-38050 Povo-Trento, Italy

机译:特伦托大学物理系生物有机化学实验室,经意大利Sovomarive 14,I-38050,Povo-Trento

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摘要

Quinolones are of clinical and scientific interest since their discovery based on the nalidixic acid in the early 1960s. They are based on two types of ring structures, the quinolone nucleus and the naphthyridone nucleus. Nalidixic acid as the first discovered agent is a naphthyridone and has only a moderate activity against Gram-negative rods. The modification of the quinolone and naphthyridone structures resulted in increasing activities of the quinolones against Gram-negative, Gram-positive, atypical and obligately anaerobic bacteria and mycobacteria. The quinolones are now divided into four groups due to their different spectrum of activity. The first and second group of quinolones i.e. norflox-acin, ciprofloxacin or ofloxacin have no or only little activity against obligately anaerobic bacteria. In contrast, the newer quinolones like sitafloxacin, clinafloxacin, trovafloxacin, moxifloxacin, gatifloxacin, garenoxacin and others like i.e. WCK 771 and ATB-492 have significant improved activities against anaerobes. Thus, these quinolones have been considered for the treatment of anaerobe and mixed infections. The present review provides an overview of the activities of quinolones against obligately anaerobic bacteria as described by in vitro as well as in vivo studies.
机译:自从1960年代初基于萘啶酸发现喹诺酮以来,就具有临床和科学意义。它们基于两种类型的环结构,喹诺酮核和萘啶酮核。萘啶酸是第一个被发现的药物,是萘啶酮,对革兰氏阴性杆菌仅具有中等活性。喹诺酮和萘啶酮结构的修饰导致喹诺酮类对革兰氏阴性,革兰氏阳性,非典型和专性厌氧细菌和分枝杆菌的活性增加。由于它们的活性谱不同,喹诺酮现在分为四类。第一组和第二组喹诺酮类药物,即诺氟沙星,环丙沙星或氧氟沙星对专性厌氧菌没有或只有很少的活性。相反,较新的喹诺酮类药物如西他沙星,clinafloxacin,trovafloxacin,moxifloxacin,gatifloxacin,garenoxacin和其他类似药物,例如WCK 771和ATB-492具有明显改善的抗厌氧菌活性。因此,已经考虑将这些喹诺酮类药物用于厌氧菌和混合感染的治疗。如体外和体内研究所述,本综述概述了喹诺酮类对专性厌氧细菌的活性。

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