title: Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
abstract: The HIV protease inhibitor Lopinavir has a pseudosymmetric core unit incorporating benzyl groups at both P-1, P-1' positions. A series of analogues incorporating non-aromatic side chains at the P-1 position were synthesized and the structure-activity relationships explored.
authors.affiliation: Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. hing.l.sham@abbott.com
authors.forename: Hing L
authors.initials: HL
authors.lastname: Sham
authors.forename: Chen
authors.initials: C
authors.lastname: Zhao
authors.forename: Leping
authors.initials: L
authors.lastname: Li
authors.forename: David A
authors.initials: DA
authors.lastname: Betebenner
authors.forename: Ayda
authors.initials: A
authors.lastname: Saldivar
authors.forename: Sudthida
authors.initials: S
authors.lastname: Vasavanonda
authors.forename: Dale J
authors.initials: DJ
authors.lastname: Kempf
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Plattner
authors.forename: Daniel W
authors.initials: DW
authors.lastname: Norbeck
mesh_terms: D002460:Cell Line; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D061466:Lopinavir; D008826:Microbial Sensitivity Tests; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D017320:HIV Protease Inhibitors; D011744:Pyrimidinones; D061466:Lopinavir