Development of Mycobacterium tuberculosis Enoyl Acyl Reductase (InhA) Inhibitors: A Mini-Review.

InhA inhibitors Mycobacterium tuberculosis SARs. antitubercular agents enoyl acyl carrier protein reductase (InhA)

Journal

Mini reviews in medicinal chemistry
ISSN: 1875-5607
Titre abrégé: Mini Rev Med Chem
Pays: Netherlands
ID NLM: 101094212

Informations de publication

Date de publication:
19 Sep 2024
Historique:
received: 12 03 2024
revised: 04 07 2024
accepted: 27 07 2024
medline: 20 9 2024
pubmed: 20 9 2024
entrez: 20 9 2024
Statut: aheadofprint

Résumé

This review article delves into the critical role of Enoyl acyl carrier protein Reductase (InhA; ENR), a vital enzyme in the NADH-dependent acyl carrier protein reductase family, emphasizing its significance in fatty acid synthesis and, more specifically, the biosynthesis of mycolic acid. The primary objective of this literature review is to elucidate diverse scaffolds and their developmental progression targeting InhA inhibition, thereby disrupting mycolic acid biosynthesis. Various scaffolds, including thiourea, piperazine, thiadiazole, triazole, quinazoline, benzamide, rhodanine, benzoxazole, and pyridine, have been systematically explored for their potential as InhA inhibitors. Noteworthy findings highlight thiadiazole and triazole derivatives, demonstrating promising IC50 values within the nanomolar concentration range. The review offers comprehensive insights into InhA's structure, structure-activity relationships, and a detailed overview of distinct scaffolds as effective inhibitors of InhA.

Identifiants

pubmed: 39301902
pii: MRMC-EPUB-143159
doi: 10.2174/0113895575309785240902102421
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Informations de copyright

Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Auteurs

Navin Kumar Tailor (NK)

University Institute of Pharma Sciences, Chandigarh University, Gharuan, Mohali, Punjab, India.

Geeta Deswal (G)

Guru Gobind Singh College of Pharmacy, Yamuna Nagar, 135001, Haryana, India.

Kumar Guarve (K)

Guru Gobind Singh College of Pharmacy, Yamuna Nagar, 135001, Haryana, India.

Ajmer Singh Grewal (AS)

Guru Gobind Singh College of Pharmacy, Yamuna Nagar, 135001, Haryana, India.

Classifications MeSH