Overview of the development of DprE1 inhibitors for combating the menace of tuberculosis

Rupesh V. Chikhale, Mahesh A. Barmade, Prashant R. Murumkar, Mange Ram Yadav

Research output: Contribution to journalArticlepeer-review

90 Citations (Scopus)


Decaprenylphosphoryl-β-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.
Original languageEnglish
Pages (from-to)8563–8593
Number of pages31
JournalJournal of Medicinal Chemistry
Issue number19
Early online date31 May 2018
Publication statusPublished - 11 Oct 2018

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