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A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation
Published on: January 9, 2019
Triterpenic Acid Amides as Potential Inhibitors of the SARS-CoV-2 Main Protease
Dmitry S Baev1, Mikhail E Blokhin1, Varvara Yu Chirkova2
1N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, 9 Lavrent'iev Avenue, 630090 Novosibirsk, Russia.
Abstract:
Although the incidence and mortality of SARS-CoV-2 infection has been declining during the pandemic, the problem related to designing novel antiviral drugs that could effectively resist viruses in the future remains relevant. As part of our continued search for chemical compounds that are capable of exerting an antiviral effect against the SARS-CoV-2 virus, we studied the ability of triterpenic acid amides to inhibit the SARS-CoV-2 main protease. Molecular modeling suggested that the compounds are able to bind to the active site of the main protease via non-covalent interactions. The FRET-based enzyme assay was used to reveal that compounds 1e and 1b can inhibit the SARS-CoV-2 main protease at micromolar concentrations.
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