Issue 61, 2020

Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective

Abstract

Tuberculosis (TB), one of the most prevalent infections, is on the rise today. Although there are drugs available in the market to combat this lethal disorder, there are several shortcomings with the current drug regimen, such as prolonged treatment period, drug resistance, high cost, etc. Hence, it is inevitable for the current researchers across the globe to embark on new strategies for TB drug discovery, which will yield highly active low cost drugs with a shorter treatment period. To achieve this, novel strategies need to be adopted to discover new drugs. Pantothenate Synthetase (PS) is one such striking drug target in Mycobacterium tuberculosis (MTB). It was observed that the pantothenate biosynthetic pathway is crucial for the pathogenicity of MTB. Pantothenate is absent in mammals and needs to be obtained from dietary sources. Hence, the pantothenate biosynthesis pathway is an impending target for emerging new therapeutics to treat TB. Worldwide, several approaches have been implemented by researchers in the quest for these inhibitors such as high-throughput screening, simulating the reaction intermediate pantoyl adenylate, use of vibrant combinatorial chemistry, hybridization approach, virtual screening of databases, inhibitors based on the crystal structure of MTB PS, etc. The present review recapitulates current developments in PS inhibitors, important analogues of numerous metabolic intermediates, and newly established inhibitors with innumerable chemical structures.

Graphical abstract: Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective

Article information

Article type
Review Article
Submitted
28 aug 2020
Accepted
30 sep 2020
First published
07 okt 2020
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2020,10, 37098-37115

Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective

A. Suresh, S. Srinivasarao, Y. M. Khetmalis, S. Nizalapur, M. Sankaranarayanan and K. V. Gowri Chandra Sekhar, RSC Adv., 2020, 10, 37098 DOI: 10.1039/D0RA07398A

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