Abstract
4,4-Dialkyl-1-hydroxy-3-oxo-3.4-dihydronaphthalene-3-yl benzothiadiazine derivatives were synthesized and evaluated as inhibitors of genotypes 1a and 1b HCV NS5B polymerase. A number of these compounds exhibited potent activity against genotypes 1a and 1b HCV polymerase in both enzymatic and cell culture activities. A representative compound also showed favorable pharmacokinetics in the rat.
MeSH terms
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Administration, Oral
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / pharmacokinetics*
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Area Under Curve
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Chemistry, Pharmaceutical / methods
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacokinetics*
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Genotype
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Infusions, Intravenous
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Inhibitory Concentration 50
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Models, Chemical
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Rats
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Viral Nonstructural Proteins / antagonists & inhibitors*
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Viral Nonstructural Proteins / genetics
Substances
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Antiviral Agents
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Enzyme Inhibitors
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Viral Nonstructural Proteins
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NS-5 protein, hepatitis C virus