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Synthesis and evaluation of heterocycle structures as potential inhibitors of Mycobacterium tuberculosis UGM

Carine Maaliki 1 Jian Fu 2 Sydney Villaume 2 Albertus Viljoen 3 Clément Raynaud 3 Sokaina Hammoud 1 Jérôme Thibonnet 1 Laurent Kremer 3 Stéphane Vincent 2 Emilie Thiery 1, *
* Corresponding author
1 SIMBA - Synthèse et isolement de molécules bio-actives EA 7502
2 UNamur - Université de Namur [Namur]
3 IRIM - Institut de Recherche en Infectiologie de Montpellier
Abstract : In this study, we screen three heterocyclic structures as potential inhibitors of UDP-galactopyranose mutase (UGM), an enzyme involved in the biosynthesis of the cell wall of Mycobacterium tuberculosis. In order to understand the binding mode, docking simulations are performed on the best inhibitors. Their activity on Mycobacterium tuberculosis is also evaluated. This study made it possible to highlight an "oxazepino-indole" structure as a new inhibitor of UGM and of M. tuberculosis growth in vitro.
Keywords : Docking Heterocycles Inhibitor Mycobacterium tuberculosis UDP-galactopyranose mutase.
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https://www.hal.inserm.fr/inserm-03082669
Contributor : Laurent Kremer <>
Submitted on : Friday, December 18, 2020 - 4:47:22 PM
Last modification on : Saturday, December 19, 2020 - 3:33:32 AM

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INSERM | SIMBA | UNIV-MONTPELLIER | UNIV-TOURS | CNRS | BS

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Carine Maaliki, Jian Fu, Sydney Villaume, Albertus Viljoen, Clément Raynaud, et al.. Synthesis and evaluation of heterocycle structures as potential inhibitors of Mycobacterium tuberculosis UGM. Bioorganic and Medicinal Chemistry, Elsevier, 2020, 28 (13), pp.115579. ⟨10.1016/j.bmc.2020.115579⟩. ⟨inserm-03082669⟩

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