Synthesis and evaluation of tripeptidyl α-ketoamides as human rhinovirus 3C protease inhibitors

We describe herein the synthesis and biological evaluation of a series of tripeptidyl alpha-ketoamides as human rhinovirus (HRV) 3C protease inhibitors. The most potent inhibitor discussed in this manuscript, 4I, exhibited impressive enzyme inhibitory activity as well as antiviral activity against H...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3531-3536
Main Authors: CHEN, Shu-Hui, LAMAR, Jason, VICTOR, Frantz, SNYDER, Nancy, JOHNSON, Robert, HEINZ, Beverly A, WAKULCHIK, Mark, WANG, Q. May
Format: Article
Language:English
Subjects:
3C Viral Proteases
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Cysteine Endopeptidases
Drug Evaluation, Preclinical
Humans
Medical sciences
Pharmacology. Drug treatments
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Structure-Activity Relationship
Viral Proteins - antagonists & inhibitors
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Summary:We describe herein the synthesis and biological evaluation of a series of tripeptidyl alpha-ketoamides as human rhinovirus (HRV) 3C protease inhibitors. The most potent inhibitor discussed in this manuscript, 4I, exhibited impressive enzyme inhibitory activity as well as antiviral activity against HRV-14.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00753-4