Design, Synthesis and Biological Evaluation of Novel SARS-CoV-2 3CLpro Covalent Inhibitors

14 September 2021, Version 3

Abstract

Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro> has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in design and synthesis which led to submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.

Keywords

COVID_19
Drug Discovery Programmes
3CLpro
SARS-CoV-2
therapeutics
antiviral

Supplementary materials

Title
Description
Actions
Title
Moitessier-Mittermaier - 3CLpro inhibitors - SuppInf
Description
Experimental data and additional information.
Actions

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