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

JiunJie Shie | Zendy; JimMin Fang | Zendy; ChihJung Kuo | Zendy; TunHsun Kuo | Zendy; PoHuang Liang | Zendy; HungJyun Huang | Zendy; WenBin Yang | Zendy; ChunHung Lin | Zendy; Jiun-Ling Chen | Zendy; Yin-Ta Wu | Zendy; ChiHuey Wong | Zendy

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

Author(s) -

JiunJie Shie,

JimMin Fang,

ChihJung Kuo,

TunHsun Kuo,

PoHuang Liang,

HungJyun Huang,

WenBin Yang,

ChunHung Lin,

Jiun-Ling Chen,

Yin-Ta Wu,

ChiHuey Wong

Publication year - 2005

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm050184y

Subject(s) - chemistry , protease , active site , enzyme inhibitor , stereochemistry , protease inhibitor (pharmacology) , residue (chemistry) , benzoic acid , non competitive inhibition , enzyme , pharmacology , biochemistry , virology , virus , medicine , antiretroviral therapy , viral load , biology

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.

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