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American Chemical Society, Journal of Medicinal Chemistry, 13(48), p. 4469-4473, 2005

DOI: 10.1021/jm050184y

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Discovery of Potent Anilide Inhibitors against the Severe Acute Respiratory Syndrome 3CL Protease

Journal article published in 2005 by Jim-Min Fang, Chih-Jung Kuo, Tun-Hsun Kuo, Po-Huang Liang, Hung-Jyun Huang, Wen-Bin Yang, Wen Bin Yang, Chun-Hung Lin, Jiun-Ling Chen, Yin-Ta Wu, Chi-Huey Wong, Jiun-Jie; Fang Jim-Min; Kuo Chih-Jung; Kuo Tun-Hsun; Liang Po-Huang; Huang Hung-Jyun; Yang Wen-Bin; Lin Chun-Hung; Chen Jiun-Ling; Wu Yin-Ta; Wong Chi-Huey Shie ORCID
This paper is available in a repository.
This paper is available in a repository.

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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.