Design, synthesis and biological evaluation of covalent peptidomimetic 3CL protease inhibitors containing nitrile moiety

Mengwei Zhu,Tiantian Fu,Mengyuan You,Junyuan Cao,Hanxi Yang, Xinyao Chen,Qiumeng Zhang,Yechun Xu,Xiangrui Jiang,Leike Zhang,Haixia Su,Yan Zhang,Jingshan Shen

Bioorganic & Medicinal Chemistry（2023）

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摘要

•A series of peptidomimetic SARS-CoV-2 3CLpro inhibitors were synthesized and evaluated.•Potent compounds were discovered by changing the P2 and P4 position.•Compounds 1a and 2b showed excellent enzyme inhibitory potency and significant antiviral activity.•The metabolic stability of 1a and 2b in liver microsomes was significantly improved.

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关键词

protease inhibitors,nitrile moiety,synthesis

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