Evaluation of heteroatom-rich derivatives as antitubercular agents with InhA inhibition properties
| Autor: | Christian Lherbet, Mohamed Amari, Beatrice Silvia Orena, Frédéric Rodriguez, Mokhtar Fodili, Nadji Belkheiri, Bachar Rébat Moulkrere, Nathalie Saffon-Merceron, Giorgia Mori, Pascal Hoffmann |
|---|---|
| Přispěvatelé: | Dipartimento di Biologia e Biotecnologie ‘Lazzaro Spallanzani’, University of Pavia, University of Pavia, Institut de Chimie de Toulouse (ICT-FR 2599), Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC), Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique (SPCMIB), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC)-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS) |
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
chemistry.chemical_classification biology 010405 organic chemistry Chemistry Stereochemistry INHA Organic Chemistry Heteroatom Fatty Acid Biosynthesis Pathway Pharmacology toxicology biology.organism_classification 01 natural sciences 3. Good health 0104 chemical sciences Mycobacterium tuberculosis 03 medical and health sciences 030104 developmental biology Enzyme Docking (molecular) [CHIM]Chemical Sciences General Pharmacology Toxicology and Pharmaceutics ComputingMilieux_MISCELLANEOUS |
| Zdroj: | Medicinal Chemistry Research Medicinal Chemistry Research, Springer Verlag, 2018, 27 (1), pp.308-320. ⟨10.1007/s00044-017-2064-x⟩ |
| ISSN: | 1054-2523 1554-8120 |
| Popis: | Two series of heterocyclic compounds derived from 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one (DHA) and 2-acetylbutyrolactone have been synthesized and characterized. The compounds were evaluated for their activities against Mycobacterium tuberculosis strain, and as inhibitors of InhA, a key enzyme involved in the type II fatty acid biosynthesis pathway of M. tuberculosis. Among the tested compounds, one DHA derivative, compound 2, showed promising activity against both mycobacteria and InhA. Docking studies were also carried out and give some new structure-activity trends compatible with current structural knowledge. |
| Databáze: | OpenAIRE |
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