Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic α, β-unsaturated esters

…, JM Fang, TH Kuo, CJ Kuo, PH Liang, HJ Huang…

Index: Shie, Jiun-Jie; Fang, Jim-Min; Kuo, Tun-Hsun; Kuo, Chih-Jung; Liang, Po-Huang; Huang, Hung-Jyun; Wu, Yin-Ta; Jan, Jia-Tsrong; Cheng, Yih-Shyun E.; Wong, Chi-Huey Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 17 p. 5240 - 5252

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Citation Number: 60

Abstract

The proteolytic processing of polyproteins by the 3CL protease of severe acute respiratory syndrome coronavirus is essential for the viral propagation. A series of tripeptide α, β- unsaturated esters and ketomethylene isosteres, including AG7088, are synthesized and assayed to target the 3CL protease. Though AG7088 is inactive (IC50> 100μM), the ketomethylene isosteres and tripeptide α, β-unsaturated esters containing both P1 and P2 ...