title: Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
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.
authors.affiliation: Pharmaceutical Discovery, D47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. hing.l.sham@abbott.com
authors.forename: H L
authors.initials: HL
authors.lastname: Sham
authors.forename: D A
authors.initials: DA
authors.lastname: Betebenner
authors.forename: T
authors.initials: T
authors.lastname: Herrin
authors.forename: G
authors.initials: G
authors.lastname: Kumar
authors.forename: A
authors.initials: A
authors.lastname: Saldivar
authors.forename: S
authors.initials: S
authors.lastname: Vasavanonda
authors.forename: A
authors.initials: A
authors.lastname: Molla
authors.forename: D J
authors.initials: DJ
authors.lastname: Kempf
authors.forename: J J
authors.initials: JJ
authors.lastname: Plattner
authors.forename: D W
authors.initials: DW
authors.lastname: Norbeck
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D002478:Cells, Cultured; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D006678:HIV / Q000187:drug effects; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D061466:Lopinavir; D008826:Microbial Sensitivity Tests; D006899:Mixed Function Oxygenases / Q000378:metabolism*; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D011744:Pyrimidinones; D061466:Lopinavir; D003577:Cytochrome P-450 Enzyme System; D006899:Mixed Function Oxygenases; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A