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Synthesis and evaluation of heterocycle structures as potential inhibitors of Mycobacterium tuberculosis UGM
- Source :
- Bioorganic and Medicinal Chemistry, Bioorganic and Medicinal Chemistry, Elsevier, 2020, 28 (13), pp.115579. ⟨10.1016/j.bmc.2020.115579⟩, Maaliki, C, Fu, J, Villaume, S, Viljoen, A, Raynaud, C, Hammoud, S, Thibonnet, J, Kremer, L, Vincent, S P & Thiery, E 2020, ' Synthesis and evaluation of heterocycle structures as potential inhibitors of Mycobacterium tuberculosis UGM ', Bioorganic and Medicinal Chemistry, vol. 28, no. 13, 115579 . https://doi.org/10.1016/j.bmc.2020.115579, Bioorganic and Medicinal Chemistry, 2020, 28 (13), pp.115579. ⟨10.1016/j.bmc.2020.115579⟩
- Publication Year :
- 2020
- Publisher :
- Elsevier, 2020.
-
Abstract
- International audience; 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.
- Subjects :
- Indoles
Tuberculosis
Inhibitor
Clinical Biochemistry
Antitubercular Agents
Drug Evaluation, Preclinical
Pharmaceutical Science
UDP-galactopyranose mutase
Microbial Sensitivity Tests
Heterocycles
010402 general chemistry
01 natural sciences
Biochemistry
Docking
Mycobacterium tuberculosis
Mutase
4-Butyrolactone
Drug Discovery
medicine
Humans
Enzyme Inhibitors
[SDV.MP] Life Sciences [q-bio]/Microbiology and Parasitology
Intramolecular Transferases
Molecular Biology
chemistry.chemical_classification
Molecular Structure
biology
010405 organic chemistry
Organic Chemistry
biology.organism_classification
medicine.disease
In vitro
3. Good health
0104 chemical sciences
Molecular Docking Simulation
Enzyme
[SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology
chemistry
Docking (molecular)
Molecular Medicine
Protein Binding
Subjects
Details
- Language :
- English
- ISSN :
- 14643391 and 09680896
- Volume :
- 28
- Issue :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganic and Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....52e14a029e53008649b1605107392fde
- Full Text :
- https://doi.org/10.1016/j.bmc.2020.115579⟩