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Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL pro Inhibitors
Author(s) -
Sun Yuanpei,
Zhang Ning,
Wang Jian,
Guo Yu,
Sun Bo,
Liu Wei,
Zhou Honggang,
Yang Cheng
Publication year - 2013
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201300392
Subject(s) - chemistry , ic50 , virtual screening , in vitro , pharmacology , structure–activity relationship , enzyme , stereochemistry , covid-19 , inhibitory postsynaptic potential , lead compound , combinatorial chemistry , biochemistry , drug discovery , medicine , disease , infectious disease (medical specialty)
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 synthetized and tested for enzymatic inhibition in vitro . Compound 1 showed potent inhibitory activity (IC 50 =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 IC 50 of 36.86 nmol/L. The structure‐activity relationships were also discussed.
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