Abstract
We describe herein the design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles.
MeSH terms
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Animals
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / pharmacology
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Dipeptides / chemical synthesis
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Dipeptides / pharmacology
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Hepacivirus / drug effects*
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Hepacivirus / enzymology
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Humans
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Male
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Proline / chemistry*
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Proline / pharmacology
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Rats
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Rats, Sprague-Dawley
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Serine Endopeptidases / metabolism*
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / pharmacology*
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Viral Nonstructural Proteins / metabolism*
Substances
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Bridged Bicyclo Compounds
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Dipeptides
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NS3 protein, hepatitis C virus
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Serine Proteinase Inhibitors
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Viral Nonstructural Proteins
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Proline
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Serine Endopeptidases