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Perspectives on SARS-CoV-2 Main Protease Inhibitors

Kaifu Gao1, Rui Wang1, Jiahui Chen1

  • 1Department of Mathematics, Michigan State University, East Lansing, Michigan 48824, United States.

Journal of Medicinal Chemistry
|November 20, 2021
PubMed

Insights

This study reviews 817 SARS-CoV-2 main protease inhibitors, analyzing their mechanisms, activity, and druggability. It highlights challenges and future directions for developing effective COVID-19 treatments targeting the viral Mpro.

Area of Science:

  • * Virology and Drug Discovery
  • * Medicinal Chemistry and Pharmacology

Background:

  • * The SARS-CoV-2 main protease (Mpro) is essential for viral replication and a key therapeutic target.
  • * Current drug development for COVID-19 is lengthy, with no approved medications yet.

Purpose of the Study:

  • * To compile and analyze a comprehensive list of SARS-CoV-2 and SARS-CoV Mpro inhibitors.
  • * To evaluate their molecular mechanisms, structure-activity relationships (SARs), antiviral activity, and druggability.

Main Methods:

  • * Literature and database compilation of 817 Mpro inhibitors.
  • * Analysis of molecular mechanisms, SARs, antiviral data, ADMET properties, and animal study results.

Main Results:

  • * Detailed review of 817 SARS-CoV and SARS-CoV-2 Mpro inhibitors.
  • * Discussion of SARs, antiviral efficacy, ADMET profiles, and animal model data.
  • * Identification of druggability and limitations for potential therapeutics.

Conclusions:

  • * The study provides a comprehensive overview of existing Mpro inhibitors.
  • * It offers insights into the development of novel inhibitors for SARS-CoV-2 and future coronavirus diseases.

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