Abstract
In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Benzamides / chemical synthesis
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Benzamides / chemistry
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Benzamides / pharmacology
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / chemistry
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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
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Bridged Bicyclo Compounds, Heterocyclic / chemistry*
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Drug Design*
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Genes, Reporter
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Hepacivirus / drug effects
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Hepacivirus / genetics
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Hepatocytes / drug effects
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Humans
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Inhibitory Concentration 50
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Oxazoles / chemical synthesis
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Oxazoles / chemistry
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Replicon
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology*
Substances
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1,4-3,6-dianhydromannitol
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Antiviral Agents
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Benzamides
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Bridged Bicyclo Compounds
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Bridged Bicyclo Compounds, Heterocyclic
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Oligopeptides
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Oxazoles
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Serine Proteinase Inhibitors