Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir)

Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir)

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. A concise synthesis of the major metabolites M-1 and M-3/ M-4 of the prote...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-06, Vol.11 (11), p.1351-1353
Hauptverfasser: Sham, Hing L, Betebenner, David A, Herrin, Thomas, Kumar, Gondi, Saldivar, Ayda, Vasavanonda, Sudthida, Molla, Akhter, Kempf, Dale J, Plattner, Jacob J, Norbeck, Daniel W
Format: Artikel
Sprache:eng
Schlagworte:
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - chemistry
Anti-HIV Agents - metabolism
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Cells, Cultured
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System - metabolism
HIV - drug effects
HIV Protease Inhibitors - chemical synthesis
HIV Protease Inhibitors - chemistry
HIV Protease Inhibitors - metabolism
HIV Protease Inhibitors - pharmacology
Humans
Lopinavir
Medical sciences
Microbial Sensitivity Tests
Mixed Function Oxygenases - metabolism
Pharmacology. Drug treatments
Pyrimidinones - chemical synthesis
Pyrimidinones - chemistry
Pyrimidinones - metabolism
Pyrimidinones - pharmacology
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Zusammenfassung: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. A concise synthesis of the major metabolites M-1 and M-3/ M-4 of the protease inhibitor ABT-378 is described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00243-8