Abstract
Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. Alpha-ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 of 340 nM.
MeSH terms
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Amides / chemistry
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Amino Acid Sequence
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Esters / chemistry
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Hepacivirus / drug effects
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Hepacivirus / metabolism
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Ketones / chemistry
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Ketones / pharmacology*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology*
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Viral Nonstructural Proteins / pharmacology*
Substances
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Amides
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Esters
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Ketones
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NS3 protein, hepatitis C virus
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Serine Proteinase Inhibitors
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Viral Nonstructural Proteins