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

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

  • Eur J Med Chem. 2020 Nov 15;206:112702. doi: 10.1016/j.ejmech.2020.112702.
Pei Liu 1,  Hongbo Liu 1,  Qi Sun 1,  Hao Liang 1,  Chunmei Li 2,  Xiaobing Deng 1,  Ying Liu 3,  Luhua Lai 4
Affiliations

Affiliations

  • 1 BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, China.
  • 2 Center for Quantitative Biology, Peking University, Beijing, 100871, China.
  • 3 BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, China; Center for Quantitative Biology, Peking University, Beijing, 100871, China. Electronic address: liuying@pku.edu.cn.
  • 4 BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, China; Center for Quantitative Biology, Peking University, Beijing, 100871, China; Peking-Tsinghua Center for Life Sciences, Peking University, Beijing, 100871, China. Electronic address: lhlai@pku.edu.cn.
PMID: 32798789 DOI: 10.1016/j.ejmech.2020.112702
Abstract

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.

Keywords

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

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