Exploring MDR-TB Inhibitory Potential of 4-Aminoquinazolines as Mycobacterium tuberculosis N-Acetylglucosamine-1-Phosphate Uridyltransferase (GlmUMTB ) Inhibitors.

Abstract

Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new antitubercular agents which operate via novel modes of action. Here, we are reporting on 4-aminoquinazolines as M. tuberculosis N-acetylglucosamine-1-phosphate uridyltransferase (GlmUMTB ) inhibitors to overcome the problem of the MDR-TB. Amongst the synthesized compounds, two of them were observed to be the effective compounds of the series (IC50 =6.4 μM (H37Rv), MIC=25 μM (MDR-TB) and IC50 =2.9 μM (H37Rv), MIC=6.25 μM (MDR-TB), respectively).

• Authors: Harun M Patel, Mahesh Palkar, Rajshekhar Karpoormath
• Journal: Chemistry & biodiversity (Chem Biodivers) Vol. 17 Issue 8 Pg. e2000237 (Aug 2020) ISSN: 1612-1880 [Electronic] Switzerland
• PMID: 32469443 (Publication Type: Journal Article)
• Copyright: © 2020 Wiley-VHCA AG, Zurich, Switzerland.

Chemical References

• 4-aminoquinazoline
• Antitubercular Agents
• Enzyme Inhibitors
• Quinazolines
• Nucleotidyltransferases
• UDPacetylglucosamine pyrophosphorylase

Topics

• Antitubercular Agents (pharmacology)
• Enzyme Inhibitors (pharmacology)
• Mycobacterium tuberculosis (drug effects)
• Nucleotidyltransferases (antagonists & inhibitors)
• Quinazolines (pharmacology)
• Spectrum Analysis (methods)
• Tuberculosis, Multidrug-Resistant (microbiology)