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

In this paper, a series of peptidomimetic SARS-CoV-2 3CL protease inhibitors with new P2 and P4 positions were synthesized and evaluated. Among these compounds, 1a and 2b exhibited obvious 3CL(pro) inhibitory activities with IC(50) of 18.06 nM and 22.42 nM, respectively. 1a and 2b also showed excell...

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Detalles Bibliográficos
Autores principales: Zhu, Mengwei, Fu, Tiantian, You, Mengyuan, Cao, Junyuan, Yang, Hanxi, Chen, Xinyao, Zhang, Qiumeng, Xu, Yechun, Jiang, Xiangrui, Zhang, Leike, Su, Haixia, Zhang, Yan, Shen, Jingshan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10166615/
https://www.ncbi.nlm.nih.gov/pubmed/37187077
http://dx.doi.org/10.1016/j.bmc.2023.117316