Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease.
Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease.
复制标题
冠状病毒3C样蛋白酶的新型拟肽抑制剂的合成及生物学评价。
DOI：
10.1016/j.ejmech.2024.116263
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发表时间：
2024
影响因子：
6.7
通讯作者：
E
中科院分区：
文献类型：
--
作者：
Amblard,Franck;LeCher,JuliaC;De,Ramyani;Zhou,Shaoman;Liu,Peng;Goh,ShuLing;Tao,Sijia;Patel,Dharmeshkumar;Downs-Bowen,Jessica;Zandi,Keivan;Zhang,Huanchun;Chaudhry,Gitika;McBrayer,Tamara;Muczynski,Michael;Al-Homoudi,Abdullah;E
严重急性呼吸系统综合征冠状病毒2（SARS-CoV-2）及其相关变体是造成2019年毁灭性冠状病毒病（COVID-19）大流行的原因。SARS-CoV-2主要蛋白酶（Mpro）在病毒复制中发挥着核心作用，并代表了一个有吸引力的药物靶点。在此，我们报告了新型SARS-CoV-2 Mpro共价抑制剂的发现，包括高效化合物NIP-22 c，其对几种关键变体和临床相关的Nirmatrelvir Mpro E166 V突变体显示出高效力。
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and related variants, are responsible for the devastating coronavirus disease 2019 (COVID-19) pandemic. The SARS-CoV-2 main protease (Mpro) plays a central role in the replication of the virus and represents an attractive drug target. Herein, we report the discovery of novel SARS-CoV-2 Mpro covalent inhibitors, including highly effective compound NIP-22cwhich displays high potency against several key variants and clinically relevant nirmatrelvir Mpro E166V mutants.