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Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2012 Jun; Vol. 52, pp. 275-83. Date of Electronic Publication: 2012 Mar 23. - Publication Year :
- 2012
-
Abstract
- A series of triazoles have been prepared and evaluated as inhibitors of InhA as well as inhibitors of Mycobacterium tuberculosis H(37)R(v). Several of these new compounds possess a good activity against InhA, particularly compounds 17 and 18 for which molecular docking has been performed. Concerning their activities against M. tuberculosis H(37)R(V) strain, two of them, 3 and 12, were found to be good inhibitors with MIC values of 0.50 and 0.25 μg/mL, respectively. Particularly, compound 12 presenting the best MIC value of all compounds tested (0.6 μM) is totally inactive against InhA.<br /> (Copyright © 2012 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antitubercular Agents chemical synthesis
Antitubercular Agents chemistry
Antitubercular Agents pharmacology
Bacterial Proteins chemistry
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Models, Molecular
Oxidoreductases chemistry
Protein Conformation
Triazoles chemistry
Bacterial Proteins antagonists & inhibitors
Mycobacterium tuberculosis drug effects
Mycobacterium tuberculosis enzymology
Oxidoreductases antagonists & inhibitors
Triazoles chemical synthesis
Triazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 52
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22483635
- Full Text :
- https://doi.org/10.1016/j.ejmech.2012.03.029