title: Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships.
abstract: The HIV protease inhibitor ABT-378 (lopinavir) has a six-member cyclic urea in the P-2 position. A series of analogues in which the six-member cyclic urea is replaced by various heterocycles was synthesized and the structure-activity relationships explored.
authors.affiliation: Pharmaceutical Discovery, R4MA 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: William
authors.initials: W
authors.lastname: Rosenbrook
authors.forename: Thomas
authors.initials: T
authors.lastname: Herrin
authors.forename: Ayda
authors.initials: A
authors.lastname: Saldivar
authors.forename: Sudthida
authors.initials: S
authors.lastname: Vasavanonda
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Plattner
authors.forename: Daniel W
authors.initials: DW
authors.lastname: Norbeck
mesh_terms: D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000737:chemistry; D006801:Humans; D061466:Lopinavir; D008826:Microbial Sensitivity Tests; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry
chemical_list: D004791:Enzyme Inhibitors; D017320:HIV Protease Inhibitors; D006571:Heterocyclic Compounds; D011744:Pyrimidinones; D061466:Lopinavir; D014508:Urea