Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis

被引:117
作者
Chikhale, Rupesh V. [1 ,2 ]
Barmade, Mahesh A. [1 ]
Murumkar, Prashant R. [1 ]
Yadav, Mange Ram [1 ]
机构
[1] Maharaja Sayajirao Univ Baroda, Fac Pharm, Kalabhavan Campus, Vadodara 390001, India
[2] Univ Manchester, Sch Hlth Sci, Div Pharm & Optometry, Manchester M13 9PL, Lancs, England
关键词
RESISTANT MYCOBACTERIUM-TUBERCULOSIS; POTENT ANTIMYCOBACTERIAL ACTIVITY; PEPTIDE DEFORMYLASE INHIBITORS; MYCOLIC ACID BIOSYNTHESIS; D-RIBOSE 2'-EPIMERASE; IN-VIVO; DRUG-RESISTANT; PYRAZINAMIDE RESISTANCE; ANTITUBERCULAR AGENTS; GENE-MUTATIONS;
D O I
10.1021/acs.jmedchem.8b00281
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Decaprenylphosphoryl-beta-D-ribose 2'-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date.
引用
收藏
页码:8563 / 8593
页数:31
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