Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL^pro Inhibitors  

作　　者：Yu Guo Ning Zhang Jian Wang Bo Sun Wei Liu Honggang Zhou Cheng Yang 

机构地区：[1]College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China [2]College of Pharmacy, Nankai University, Tianjin 300071, China [3]College of Life Sciences, Nankai University, Tianjin 300071, China [4]High Throughput Molecular Drug Discovery Center, Tianjin International Joint Academy of Biotechnology and Medicine, TEDA, Tianjin 300457, China

出　　处：《Chinese Journal of Chemistry》2013年第9期1199-1206,共8页中国化学（英文版）

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.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.

关 键 词：SARS SARS CoV 3CL^pro INHIBITORS QUINOLINONE 

分 类 号：TQ655[化学工程—精细化工] R373[医药卫生—病原生物学]