Screening of electrophilic compounds yields an aziridin, as new active-site directed SARS-CoV main protease inhibitor

[摘要] 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 revealec 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. (c) 2005 Elsevier Ltd. All rights reserved.

[发布日期] 2005-12-15

[关键词] SARS;main protease;inhibitor;aziridine