Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL^pro Inhibitors
Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL^pro Inhibitors作者机构：College of Sciences Tianjin University of Science and Technology Tianjin 300457 China College of Pharmacy Nankai University Tianjin 300071 China College of Life Sciences Nankai University Tianjin 300071 China High Throughput Molecular Drug Discovery Center Tianjin International Joint Academy of Biotechnology and Medicine TEDA Tianjin 300457 China
出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)
年 卷 期：2013年第31卷第9期
页 面：1199-1206页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 100705[医学-微生物与生化药学] 081702[工学-化学工艺] 1001[医学-基础医学(可授医学、理学学位)] 08[工学] 0817[工学-化学工程与技术] 100103[医学-病原生物学] 10[医学]
基 金：supported by Tianjin SME TEchnology Innovation Fund National Biomedical Special Project of International Innovation Park
主 题：SARS SARS CoV 3CL^pro inhibitors quinolinone
摘 要：SARS CoV 3CL^pro is known to be a promising target for development of therapeutic agents against the severe acute respiratory syndrome （SARS）. A quinolinone compound 1 was selected via virtual screening, and it was syn- thetized and tested for enzymatic inhibition in vitro. Compound 1 showed potent inhibitory activity （ICs0= 0.44 μmol/L） toward SARS CoV 3CL^pro. Further work on a series of quinolinone derivatives resulted in the discovery of the most potent compound 23, inhibiting SARS CoV 3CL^pro with an IC50 of 36.86 μmol/L. The structure-activity relationships were also discussed.
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