Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CLpro Inhibitors
Yuanpei Sun, Ning Zhang, Jian Wang, Yu Guo, Bo Sun, Wei Liu, Honggang Zhou, Cheng Yang · Chinese Journal of Chemistry · 2013
Abstract SARS CoV 3CLpro 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 synthetized and tested for enzymatic inhibition in vitro. Compound 1 showed potent inhibitory activity (IC50=0.44 µmol/L) toward SARS CoV 3CLpro. Further work on a series of quinolinone derivatives resulted in the discovery of the most potent compound 23, inhibiting SARS CoV 3CLpro with an IC50 of 36.86 nmol/L. The structure‐activity relationships were also discussed.