Fragment-based approaches to TB drugs

被引:15
|
作者
Marchetti, Chiara [1 ]
Chan, Daniel S. H. [1 ]
Coyne, Anthony G. [1 ]
Abell, Chris [1 ]
机构
[1] Univ Cambridge, Dept Chem, Lensfield Rd, Cambridge CB2 1EW, England
关键词
tuberculosis; fragment-based approaches; medicinal chemistry; cytochrome P450; pantothenate synthetase; EthR; BioA; MYCOBACTERIUM-TUBERCULOSIS CYP121; SMALL-MOLECULE INHIBITORS; PANTOTHENATE SYNTHETASE; ETHIONAMIDE BOOSTERS; ETHR INHIBITORS; DISCOVERY; CYTOCHROME-P450; IDENTIFICATION; REPRESSOR; ANTIGEN;
D O I
10.1017/S0031182016001876
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
Tuberculosis is an infectious disease associated with significant mortality and morbidity worldwide, particularly in developing countries. The rise of antibiotic resistance in Mycobacterium tuberculosis (Mtb) urgently demands the development of new drug leads to tackle resistant strains. Fragment-based methods have recently emerged at the forefront of pharmaceutical development as a means to generate more effective lead structures, via the identification of fragment molecules that form weak but high quality interactions with the target biomolecule and subsequent fragment optimization. This review highlights a number of novel inhibitors of Mtb targets that have been developed through fragment-based approaches in recent years.
引用
收藏
页码:184 / 195
页数:12
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