4.7 Article

Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 206, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112702

Keywords

COVID-19; SARS-CoV-2 3C-like protease; N-substituted isatin compounds; In vitro assay; Structure-activity relationship

Funding

  1. National Natural Science Foundation of China [21633001,21877003]
  2. Ministry of Science and Technology of China [2016YFA0502303]

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SARS-CoV-2 3C like protease is the main protease of SARS-CoV-2 and has been considered as one of the key targets for drug discovery against COVID-19. We identified several N-substituted isatin compounds as potent SARS-CoV-2 3C-like protease inhibitors. The three most potent compounds inhibit SARS-CoV-2 3C-like protease with IC50's of 45 nM, 47 nM and 53 nM, respectively. Our study indicates that N-substituted isatin compounds have the potential to be developed as broad-spectrum anti-coronavirus drugs. (C) 2020 Elsevier Masson SAS. All rights reserved.

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