2. Academic Validation
  3. Fluoroquinolone derivatives and their anti-tubercular activities

Fluoroquinolone derivatives and their anti-tubercular activities

  • Eur J Med Chem. 2018 Feb 25:146:554-563. doi: 10.1016/j.ejmech.2018.01.080.
Yi-Lei Fan 1,  Jian-Bing Wu 2,  Xiang-Wei Cheng 2,  Feng-Zhi Zhang 3,  Lian-Shun Feng 4
Affiliations

Affiliations

  • 1 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.
  • 2 Key Laboratory of Drug Prevention and Control Technology of Zhejiang Province, Zhejiang Police College, Hangzhou, PR China.
  • 3 College of Pharmaceutical Science & Green Pharmaceutical Collaborative Innovation Center of Yangtze River Delta Region, Zhejiang University of Technology, Hangzhou, 310014, PR China. Electronic address: zhangfengzhi@zjut.edu.cn.
  • 4 Synthetic and Functional Biomolecules Center, Peking University, Beijing, PR China.
PMID: 29407980 DOI: 10.1016/j.ejmech.2018.01.080
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.

Keywords

Anti-mycobacterial; Anti-tubercular; Fluoroquinolones; Structure-activity relationship.

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