Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease
Resource
Journal of medicinal chemistry 48: 4469-4473
Journal
Journal of Medicinal Chemistry
Journal Volume
48
Journal Issue
13
Pages
4469-4473
Date Issued
2005
Author(s)
Shie, Jiun-Jie
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.
SDGs
Type
journal article
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