Synthesis, biological evaluation and computational studies of pyrazole derivatives as <i>Mycobacterium tuberculosis</i> CYP121A1 inhibitors-Reference-Cited by-同舟云学术

Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors

Published:2022 Issue:11 Volume:13 Page:1350-1360
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Alshabani Lama A.¹,Kumar Amit²^ORCID,Willcocks Sam J.³⁴,Srithiran Gayathri⁴,Bhakta Sanjib⁴,Estrada D. Fernando²,Simons Claire¹^ORCID

Affiliation:

1. School of Pharmacy & Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3NB UK

2. Department of Biochemistry, Jacobs School of Medicine and Biomedical Science, University at Buffalo, Buffalo, New York-14203, USA

3. Department of Infection Biology, The London School of Hygiene and Tropical Medicine, London, WC1E 7HT UK

4. Mycobacteria Research Laboratory, Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London, London WC1E 7HX, UK

Abstract

Pyrazole derivatives were evaluated using UV-vis and protein-detected 1D 19F-NMR (Mtb CYP121A1 binding affinity), antimycobacterial determination (MIC) and computational studies illustrating the potential anti-TB properties of the compounds.

Funder

Princess Nourah Bint Abdulrahman University

European Regional Development Fund

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D2MD00155A

Reference26 articles.

1. World Health Organisation, Global tuberculosis report 2021, https://www.who.int/publications/i/item/9789240037021 , (accessed 23 March 2022)

2. Drug resistant Tuberculosis: A review