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

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 mu M) for SARS CoV and 5.2 log (at 1.25 mu M) for...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 49; no. 16; pp. 4971 - 4980
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	WASHINGTON Amer Chemical Soc 10.08.2006
Subjects:	Animals Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Carbamates - chemical synthesis Carbamates - chemistry Carbamates - pharmacology Cell Line Chemistry, Medicinal Chlorocebus aethiops Coronavirus 229E, Human - drug effects Crystallography, X-Ray Cysteine Endopeptidases - chemistry Dipeptides - chemical synthesis Dipeptides - chemistry Dipeptides - pharmacology Drug Stability Humans Hydrogen Bonding Hydrophobic and Hydrophilic Interactions Life Sciences & Biomedicine Mice Models, Molecular Molecular Structure Pharmacology & Pharmacy Rats SARS Virus - drug effects Science & Technology Structure-Activity Relationship Viral Proteins - antagonists & inhibitors Viral Proteins - chemistry Virus Replication - drug effects DESIGN GENOME SEQUENCE VIRUS ACUTE RESPIRATORY SYNDROME PROGRAM
ISSN:	0022-2623, 1520-4804
Online Access:	Get more information
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