Eur J Med Chem . 2 Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds

[tetano]

Eur J Med Chem


. 2020 Aug 1;206:112702.
doi: 10.1016/j.ejmech.2020.112702. Online ahead of print.
Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds


Pei Liu[SUP] 1 [/SUP], Hongbo Liu[SUP] 1 [/SUP], Qi Sun[SUP] 1 [/SUP], Hao Liang[SUP] 1 [/SUP], Chunmei Li[SUP] 2 [/SUP], Xiaobing Deng[SUP] 1 [/SUP], Ying Liu[SUP] 3 [/SUP], Luhua Lai[SUP] 4 [/SUP]



Affiliations

• PMID: 32798789
• PMCID: PMC7395831
• 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 IC[SUB]50[/SUB]'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.