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Synthesis of New Binary Thiazole-Based Heterocycles and Their Molecular Docking Study as COVID-19 Main Protease (Mpro) Inhibitors

Ehab Abdel‐Latif, Tamer K. Khatab, Ahmed Fekri, Mohamed E. Khalifa

2021Russian Journal of General Chemistry19 citationsDOIOpen Access PDF

Abstract

Isolated polynuclear binary heterocyclic compounds containing thiazole building block combined with benzofuran, pyrrole, thiazole, or thiophene via carboxamide and/or secondary amine as a junction are presented. The synthetic strategy of those is based on utilization of 2-chloroacetamido-4-phenylthiazole in the synthesis of binary heterocyclic compounds by cyclocondensation with salicylic aldehyde, acetonitrile derivatives, ammonium thiocyanate, 3-mercaptoacrylonitrile derivatives, and/or 3-mercaptoacrylate derivatives. The prepared binary thiazole-based heterocycles have been studied as protease (Mpro) inhibitors by molecular docking for visualization of their orientation and interactions with COVID-19 units using hydroxychloroquine as a reference molecule.

Topics & Concepts

ChemistryThiazoleCombinatorial chemistryDocking (animal)AcetonitrileBenzofuranStereochemistryOrganic chemistryMedicineNursingSynthesis and biological activitySynthesis and Characterization of Heterocyclic CompoundsMulticomponent Synthesis of Heterocycles