Abstract
The first series of peptidyl aldehyde inhibitors that incorporate in their structure a glutamine surrogate has been designed and synthesized based on the known substrate specificity of Norwalk virus 3C protease. The inhibitory activity of the compounds with the protease and with a norovirus cell-based replicon system was investigated. Members of this class of compounds exhibited noteworthy activity both in vitro and in a cell-based replicon system.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Chemistry Techniques, Synthetic
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Crystallography, X-Ray
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Cysteine Proteases / metabolism*
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Cysteine Proteinase Inhibitors / chemical synthesis*
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Cysteine Proteinase Inhibitors / chemistry
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Cysteine Proteinase Inhibitors / pharmacology*
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Dose-Response Relationship, Drug
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Drug Design*
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Models, Molecular
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Molecular Conformation
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Norwalk virus / enzymology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cysteine Proteinase Inhibitors
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Cysteine Proteases