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J Med Chem. 2005 Jun 30;48(13):4469-73.

Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.

Author information

1
Department of Chemistry, National Taiwan University, Taipei, 106, Taiwan.

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.

PMID:
15974598
DOI:
10.1021/jm050184y
[Indexed for MEDLINE]

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