Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor

…, HC Chen, CW Kuo, CS Wu, LW Chang…

文献索引：Yang, Syaulan; Chen, Shu-Jen; Hsu, Min-Feng; Wu, Jen-Dar; Tseng, Chien-Te K.; Liu, Yu-Fan; Chen, Hua-Chien; Kuo, Chun-Wei; Wu, Chi-Shen; Chang, Li-Wen; Chen, Wen-Chang; Liao, Shao-Ying; Chang, Teng-Yuan; Hung, Hsin-Hui; Shr, Hui-Lin; Liu, Cheng-Yuan; Huang, Yu-An; Chang, Ling-Yin; Hsu, Jen-Chi; Peters, Clarence J.; Wang, Andrew H.-J.; Hsu, Ming-Chu Journal of Medicinal Chemistry, 2006 ,  vol. 49,  # 16  p. 4971 - 4980

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被引用次数: 48

摘要

A potent SARS coronavirus (CoV) 3CL protease inhibitor (TG-0205221, K i= 53 nM) has been developed. TG-0205221 showed remarkable activity against SARS CoV and human coronavirus (HCoV) 229E replications by reducing the viral titer by 4.7 log (at 5 μM) for SARS CoV and 5.2 log (at 1.25 μM) for HCoV 229E. The crystal structure of TG-0205221 (resolution= 1.93 Å) has revealed a unique binding mode comprising a covalent bond, ...