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-3H-pyrazol-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.