Design and Synthesis of Some New Benzothiazolyl-pyrazole Derivatives as Potential Anti-dengue Agents

Mohd Zaheen Hassan, Abdulrhman Alsayari, Yahya I. Asiri, Abdullatif Bin Muhsinah, Mehnaz Kamal

Research output: Contribution to journalArticlepeer-review

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 languageEnglish
Pages (from-to)29-33
Number of pages5
JournalIndian Journal of Heterocyclic Chemistry
Volume32
Issue number1
StatePublished - Mar 2022

Keywords

  • Benzothiazole
  • Dengue
  • Molecular docking
  • Protease
  • Pyrazole

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