Abstract
Prolonged hepatitis C infection is the leading cause for cirrhosis of the liver and hepatocellular carcinoma. The etiological agent HCV virus codes a single polyprotein of approximately 3000 amino acids that is processed with the help of a serine protease NS3A to produce structural and non-structural proteins required for viral replication. Inhibition of NS3 protease can potentially be used to develop drugs for treatment of HCV infections. Herein, we report the development of a series of novel NS3 serine protease inhibitors derived from 2-aza-bicyclo[2.2.1]-heptane carboxylic acid with potential therapeutic use for treatment of HCV infections.
MeSH terms
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Binding Sites
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Bridged Bicyclo Compounds* / chemical synthesis
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Bridged Bicyclo Compounds* / chemistry
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Bridged Bicyclo Compounds* / pharmacology
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Hepacivirus / chemistry
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Hepacivirus / drug effects*
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Hepacivirus / enzymology
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Molecular Structure
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Protein Binding
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Replicon / drug effects*
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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
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Structure-Activity Relationship
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Viral Nonstructural Proteins / antagonists & inhibitors*
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Viral Nonstructural Proteins / chemistry
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X-Ray Diffraction
Substances
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2-azabicyclo(2.2.1)heptane-3-carboxylic acid
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Bridged Bicyclo Compounds
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NS3 protein, hepatitis C virus
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Serine Proteinase Inhibitors
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Viral Nonstructural Proteins