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Design, synthesis and biological evaluation of novel triazole, urea and thiourea derivatives of quinoline against Mycobacterium tuberculosis
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2009 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 17, no 13, 4681-4692 p.Article in journal (Refereed) Published
Abstract [en]

A new series of 20 quinoline derivatives possessing triazolo, ureido and thioureido substituents have been synthesized and their antimycobacterial properties have been evaluated. Compounds 10, 22 and 24 inhibited Mycobacterium tuberculosis H37Rv up to 96%, 98% and 94% respectively, at a fixed concentration of 6.25 mu g/mL. Minimum inhibitory concentration of 3.125 mu g/mL was obtained for compound 10 and 24, while for compound 22 it was 6.25 mu g/mL. Molecular docking calculations suggest critical hydrogen bonding and electrostatic interactions between polar functional groups (such as quinoline-nitrogen, urea-carbonyl and hydroxyl) of anti-mycobacterial (anti-TB) compounds and amino acids (Arg186 and Glu61) of ATP-synthase of M. tuberculosis, could be the probable reason for observed anti-mycobacterial action. (C) 2009 Elsevier Ltd. All rights reserved.

Place, publisher, year, edition, pages
2009. Vol. 17, no 13, 4681-4692 p.
Keyword [en]
Tuberculosis, ATP synthase, Diarylquinoline, Anti-tuberculosis (anti-TB) drugs
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-129002DOI: 10.1016/j.bmc.2009.04.069ISI: 000266822900045OAI: oai:DiVA.org:uu-129002DiVA: diva2:332429
Available from: 2010-08-05 Created: 2010-08-05 Last updated: 2010-08-05Bibliographically approved

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