title: Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
abstract: The HIV protease inhibitor ABT-378 (Lopinavir) has a 2,6-dimethylphenoxyacetyl group in the P-2' position. Analogues in which this group is replaced with various substituted phenyl or heteroaryl groups were synthesized and the structure-activity relationships explored.
authors.affiliation: Pharmaceutical Discovery, D47B, 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: David A
authors.initials: DA
authors.lastname: Betebenner
authors.forename: Xiaoqi
authors.initials: X
authors.lastname: Chen
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* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D061466:Lopinavir; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D017320:HIV Protease Inhibitors; D011744:Pyrimidinones; D061466:Lopinavir