ATP Synthase, an Emerging Target in TB Drug Discovery: Review of SAR and Clinical Pharmacology of Diarylquinoline Inhibitors

Author(s): Abhijeet Dhulap*, Paromita Banerjee

Journal Name: Current Drug Targets

Volume 22 , Issue 11 , 2021

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Graphical Abstract:


Tuberculosis (TB) caused by Mycobacterium tuberculosis (MTB) is one of the leading causes of mortality worldwide, with an estimated 1.5 million deaths annually. The majority of infection cases are reported from the Southeast Asian region, including India. After the discovery of Streptomycin in 1943 and its anti-tubercular activity in 1945, drug discovery efforts identified Isoniazid, Ethambutol, and Rifampin as TB-actives. However, over the years, these drugs have been rendered ineffective due to genetic mutations in mycobacterial strains. This has shifted drug discovery efforts towards identifying new targets and drugs for drug-resistant forms of bacteria. ATP synthase was identified as one of the key targets of MDR-TB. This review provides key insights into the ATP synthase target, structure activity relationship studies (SAR) of diarylquinoline class of inhibitors and their clinical relevance for treating MDR-TB.

Keywords: ATP synthase, tuberculosis, diarylquinoline, bedaquiline, mycobacterial, drug target.

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Article Details

Year: 2021
Published on: 21 January, 2021
Page: [1207 - 1221]
Pages: 15
DOI: 10.2174/1389450122666210122084332
Price: $65

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PDF: 52