Abstract
Synthesis and SAR of 2-alkyloxazoles as class III phosphatidylinositol-4-kinase beta (PI4KIIIβ) inhibitors is described. These compounds demonstrate that inhibition of PI4KIIIβ leads to potent inhibition of HCV replication as observed in genotype (GT) 1a and 1b replicon and GT2a JFH1 virus assays in vitro.
Keywords:
HCV; PI4K.
Copyright © 2014 Elsevier Ltd. All rights reserved.
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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Dose-Response Relationship, Drug
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Hepacivirus / drug effects*
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Hepacivirus / enzymology
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Humans
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Microbial Sensitivity Tests
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Molecular Structure
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Oxazoles / chemical synthesis
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Oxazoles / chemistry
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Oxazoles / pharmacology*
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Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*
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Phosphotransferases (Alcohol Group Acceptor) / metabolism
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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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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Oxazoles
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Protein Kinase Inhibitors
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Phosphotransferases (Alcohol Group Acceptor)