4.3 Article

Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors

Journal

CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 56, Issue 10, Pages 1400-1405

Publisher

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.1400

Keywords

SARS coronavirus 3CL protease; cinanserin analogs; inhibitor; fluorescence resonance energy transfer-based assay

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The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the in-hibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC50 of 1.06 mu M.

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