title: Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors.
abstract: The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC(50) of 1.06 microM.
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
authors.forename: Qingang
authors.initials: Q
authors.lastname: Yang
authors.forename: Lili
authors.initials: L
authors.lastname: Chen
authors.forename: Xuchang
authors.initials: X
authors.lastname: He
authors.forename: Zhenting
authors.initials: Z
authors.lastname: Gao
authors.forename: Xu
authors.initials: X
authors.lastname: Shen
authors.forename: Donglu
authors.initials: D
authors.lastname: Bai
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002928:Cinanserin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D000086782:Coronavirus 3C Proteases; D003546:Cysteine Endopeptidases; D015195:Drug Design; D031541:Fluorescence Resonance Energy Transfer; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D045473:Severe acute respiratory syndrome-related coronavirus / Q000201:enzymology*; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014764:Viral Proteins / Q000037:antagonists & inhibitors*
chemical_list: D000998:Antiviral Agents; D007202:Indicators and Reagents; D011480:Protease Inhibitors; D012702:Serotonin Antagonists; D014764:Viral Proteins; D003546:Cysteine Endopeptidases; D000086782:Coronavirus 3C Proteases; D002928:Cinanserin