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ID: ALA1141957
Journal: Bioorg Med Chem Lett
Title: Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
Authors: Martina E, Stiefl N, Degel B, Schulz F, Breuning A, Schiller M, Vicik R, Baumann K, Ziebuhr J, Schirmeister T.
Abstract: The coronavirus main protease, M(pro), is considered a major target for drugs suitable to combat coronavirus infections including the severe acute respiratory syndrome (SARS). In this study, comprehensive HPLC- and FRET-substrate-based screenings of various electrophilic compounds were performed to identify potential M(pro) inhibitors. The data revealed that the coronaviral main protease is inhibited by aziridine- and oxirane-2-carboxylates. Among the trans-configured aziridine-2,3-dicarboxylates the Gly-Gly-containing peptide 2c was found to be the most potent inhibitor.
CiteXplore: 16216498