Abstract
The HIV protease inhibitor ABT-378 (Lopinavir) is metabolized rapidly and extensively by CYP-3A4 catalyzed oxidation. Three of the major metabolites identified were synthesized and their antiviral (HIV) activities determined.
MeSH terms
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / metabolism
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Anti-HIV Agents / pharmacology
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Cells, Cultured
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme System / metabolism*
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HIV / drug effects
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HIV Protease Inhibitors / chemical synthesis*
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HIV Protease Inhibitors / chemistry
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HIV Protease Inhibitors / metabolism
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HIV Protease Inhibitors / pharmacology
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Humans
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Lopinavir
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Microbial Sensitivity Tests
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Mixed Function Oxygenases / metabolism*
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Pyrimidinones / chemical synthesis
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Pyrimidinones / chemistry
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Pyrimidinones / metabolism*
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Pyrimidinones / pharmacology
Substances
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Anti-HIV Agents
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HIV Protease Inhibitors
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Pyrimidinones
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Lopinavir
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Cytochrome P-450 Enzyme System
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Mixed Function Oxygenases
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CYP3A protein, human
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Cytochrome P-450 CYP3A