Synthesis and Biological Evaluation of Quinolinone Compounds as SARS CoV 3CL^pro Inhibitors
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...
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Veröffentlicht in: | Chinese journal of chemistry 2013-09, Vol.31 (9), p.1199-1206 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | 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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ISSN: | 1001-604X 1614-7065 |
DOI: | 10.1002/cjoc.201300392 |