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氟喹诺酮衍生物及其抗结核活性。

Fluoroquinolone derivatives and their anti-tubercular activities.

作者信息

Fan Yi-Lei, Wu Jian-Bing, Cheng Xiang-Wei, Zhang Feng-Zhi, Feng Lian-Shun

机构信息

College of Pharmaceutical Science & Green Pharmaceutical Collaborative Innovation Center of Yangtze River Delta Region, Zhejiang University of Technology, Hangzhou, 310014, PR China; Key Laboratory of Drug Prevention and Control Technology of Zhejiang Province, Zhejiang Police College, Hangzhou, PR China.

Key Laboratory of Drug Prevention and Control Technology of Zhejiang Province, Zhejiang Police College, Hangzhou, PR China.

出版信息

Eur J Med Chem. 2018 Feb 25;146:554-563. doi: 10.1016/j.ejmech.2018.01.080. Epub 2018 Jan 31.

Abstract

Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, around one-third of the world's population harbor a latent infection by Mycobacterium tuberculosis (MTB), and 5-10% eventually develop an active TB. The emergency of MTB new virulent forms as well as the co-infection between MTB and HIV alarming the serious problem in TB control and demanding the need for new drugs more potent than earlier with safe ADME profile. Fluoroquinolones are emerged as a large family of synthetic broad spectrum antibiotics, and some of them were recommended as the second-line agents for the treatment of TB mainly in cases involving resistance or intolerance to first-line anti-TB therapy by WHO. Numerous of FQs derivatives have been synthesized for seeking for new anti-TB agents, and some of them exhibited promising potency. This review aims to summarize the recent advances made towards the discovery of FQs derivatives as anti-TB agents and the structure-activity relationship of these derivatives.

摘要

结核病(TB)仍然是最广泛传播且致死率最高的疾病之一,全球约三分之一的人口潜伏感染结核分枝杆菌(MTB),其中5%-10%最终会发展为活动性结核病。MTB新的致病形式的出现以及MTB与HIV的合并感染,警示着结核病控制中的严重问题,并且需要比早期药物更有效且具有安全的药代动力学和毒理学特性的新药。氟喹诺酮类药物是一大类合成的广谱抗生素,其中一些被世界卫生组织推荐作为二线药物,主要用于治疗对一线抗结核治疗耐药或不耐受的结核病患者。为了寻找新的抗结核药物,人们合成了大量氟喹诺酮类衍生物,其中一些显示出了有前景的活性。这篇综述旨在总结氟喹诺酮类衍生物作为抗结核药物的研究进展及其构效关系。

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