Banerjee, Deb Ranjan ; Senapati, Kalyan ; Biswas, Rupam ; Das, Amit K. ; Basak, Amit (2015) Inhibition of M. tuberculosis β-ketoacyl CoA reductase FabG4 (Rv0242c) by triazole linked polyphenol–aminobenzene hybrids: Comparison with the corresponding gallate counterparts Bioorganic & Medicinal Chemistry Letters, 25 (6). pp. 1343-1347. ISSN 0960-894X
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Official URL: http://doi.org/10.1016/J.Bmcl.2015.01.014
Related URL: http://dx.doi.org/10.1016/J.Bmcl.2015.01.014
Abstract
Herein we report six novel triazole linked polyphenol-aminobenzene hybrids (3-8) as inhibitors of Mycobacterium tuberculosis FabG4 (Rv0242c), a less explored β-ketoacyl CoA reductase that has immense potential to be the future anti-tuberculosis drug target due to its possible involvement in drug resistance and latent infection. Novel triazole linked polyphenol-aminobenzene hybrids have been synthesized, characterized and evaluated for their inhibitory activity against FabG4. All of them inhibit FabG4 at low micromolar concentrations. In silico docking study has been carried out to explain the experimental findings. A comparative study of these new inhibitors with previously reported gallate counterparts leads to structure-activity relations (SAR) of substituent linked to N-1 of triazole ring.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | FabG4; Fatty acid synthesis; Inhibition; Micromolar; SAR; Tuberculosis. |
| ID Code: | 130020 |
| Deposited On: | 02 Dec 2022 06:02 |
| Last Modified: | 05 Dec 2022 05:43 |
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