Abstract
Hepatitis C virus (HCV) infection represents a serious health-care problem. Previously we reported the identification of NA255 from our natural products library using a HCV sub-genomic replicon cell culture system. Herein, we report how the absolute stereochemistry of NA255 was determined and an enantioselective synthetic method for NA255 derivatives was developed. The structure-activity relationship of the NA255 derivatives and rat pharmacokinetic profiles of the representative compounds are disclosed.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / pharmacokinetics
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Antiviral Agents / toxicity
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Cell Line
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Cell Survival / drug effects
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Citrates / chemistry*
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Citrates / pharmacokinetics
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Citrates / toxicity
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Half-Life
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Hepacivirus / drug effects
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Hepacivirus / growth & development*
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Humans
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Phenylpropionates / chemistry*
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Phenylpropionates / pharmacokinetics
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Phenylpropionates / toxicity
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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Antiviral Agents
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Citrates
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NA 255
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Phenylpropionates