Abstract
Dengue is a serious mosquito-borne viral disease, causing millions of death worldwide. Herein, we report the design, synthesis, and protease inhibitory activity of pyrazole containing benzothiazole scaffold. A series of benzothiazolyl-pyrazoles (1a-i) was synthesized by the one-pot three-component reaction of ethyl acetoacetate, 6-bromo-2-hydrazinylbenzothiazole, and aryldiazonium salts under solvent-free conditions. In silico screening of these compounds against DENV2 NS2B/NS3 protease revealed, 2-(6-bromobenzothiazol-2-yl)-5-methyl-4-[2-(p-tolyl)hydrazono]-2,4-dihydro-3Hpyrazol- 3-one (1b) as a promising anti-dengue agent acting through dengue protease inhibition. Thus, pyrazolyl analogs containing benzothiazole nucleus could provide a potential lead for the development of novel anti-dengue agents.
Original language | English |
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Pages (from-to) | 29-33 |
Number of pages | 5 |
Journal | Indian Journal of Heterocyclic Chemistry |
Volume | 32 |
Issue number | 1 |
State | Published - Mar 2022 |
Keywords
- Benzothiazole
- Dengue
- Molecular docking
- Protease
- Pyrazole