4.5 Article

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

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CHEMISTRY & BIODIVERSITY
卷 17, 期 8, 页码 -

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.202000237

关键词

4-aminoquinazoline; N-acetylglucosamine-1-phosphate uridyltransferase (GlmU(MTB))MDR-TB; cytotoxicity

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  1. Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, South Africa

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Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new antitubercular agents which operatevianovel modes of action. Here, we are reporting on 4-aminoquinazolines asM. tuberculosis N-acetylglucosamine-1-phosphate uridyltransferase (GlmU(MTB)) 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 mu M (H37Rv), MIC=25 mu M (MDR-TB) and IC50=2.9 mu M (H37Rv), MIC=6.25 mu M (MDR-TB), respectively).

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