| Literature DB >> 15974598 |
Jiun-Jie Shie1, Jim-Min Fang, Chih-Jung Kuo, Tun-Hsun Kuo, Po-Huang Liang, Hung-Jyun Huang, Wen-Bin Yang, Chun-Hung Lin, Jiun-Ling Chen, Yin-Ta Wu, Chi-Huey Wong.
Abstract
A diversified library of peptide anilides was prepared, and their inhibition activities against the SARS-CoV 3CL protease were examined by a fluorogenic tetradecapeptide substrate. The most potent inhibitor is an anilide derived from 2-chloro-4-nitroaniline, l-phenylalanine and 4-(dimethylamino)benzoic acid. This anilide is a competitive inhibitor of the SARS-CoV 3CL protease with K(i) = 0.03 muM. The molecular docking experiment indicates that the P1 residue of this anilide inhibitor is distant from the nucleophilic SH of Cys145 in the active site.Entities:
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Year: 2005 PMID： 15974598 DOI： 10.1021/jm050184y
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446