The identification of α-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase

Peptides based upon the non-prime side residues of the NS4A-4B cleavage site of hepatitis C virus (HCV) NS3-4A proteinase containing an alpha-ketoamide moiety in place of the scissile amide bond are potent inhibitors of this enzyme.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (3), p.355-357
Main Authors: BENNETT, J. M, CAMPBELL, A. D, KAY, P. B, O'BRIEN, M. A, KING-UNDERWOOD, J, RAYNHAM, T. M, WILKINSON, C. S, WILKINSON, T. C. I, WILSON, F. X, CAMPBELL, A. J, CARR, M. G, DUNSDON, R. M, GREENING, J. R, HURST, D. N, JENNINGS, N. S, JONES, P. S, JORDAN, S
Format: Article
Language:English
Subjects:
Amides - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemical synthesis
Antiviral Agents - pharmacology
Biological and medical sciences
Combinatorial Chemistry Techniques
Humans
Inhibitory Concentration 50
Medical sciences
Molecular Mimicry
Peptides - chemical synthesis
Peptides - pharmacology
Pharmacology. Drug treatments
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - pharmacology
Structure-Activity Relationship
Viral Nonstructural Proteins - antagonists & inhibitors
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Description
Summary:Peptides based upon the non-prime side residues of the NS4A-4B cleavage site of hepatitis C virus (HCV) NS3-4A proteinase containing an alpha-ketoamide moiety in place of the scissile amide bond are potent inhibitors of this enzyme.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00654-5