A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors*.

ABSTRACT: The COVID-19 pathogen, SARS-CoV-2, requires its main protease (SC2M^Pro ) to digest two of its translated long polypeptides to form a number of mature proteins that are essential for viral replication and pathogenesis. Inhibition of this vital proteolytic process is effective in preventing the virus from replicating in infected cells and therefore provides a potential COVID-19 treatment option. Guided by previous medicinal chemistry studies about SARS-CoV-1 main protease (SC1M^Pro ), we have designed and synthesized a series of SC2M^Pro inhibitors that contain β-(S-2-oxopyrrolidin-3-yl)-alaninal (Opal) for the formation of a reversible covalent bond with the SC2M^Pro active-site cysteine C145. All inhibitors display high potency with K_i va

SUBMITTER: Yang KS 

PROVIDER: S-EPMC7979488 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature