Author: Sun, Yuanpei; Zhang, Ning; Wang, Jian; Guo, Yu; Sun, Bo; Liu, Wei; Zhou, Honggang; Yang, Cheng
Title: Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL(pro) Inhibitors Cord-id: ew6kqsfr Document date: 2013_7_19
ID: ew6kqsfr
Snippet: 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
Document: 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 structureâ€activity relationships were also discussed.
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