title: Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
abstract: As part of our efforts to identify potent HIV-1 protease inhibitors that are active against resistant viral strains, structural modification of the azacyclic urea (I) was undertaken by incorporating acyl groups as P(1)' ligands. The extensive SAR study has yielded a series of N-acyl azacyclic ureas (II), which are highly potent against both wild-type and multiple PI-resistant viral strains.
authors.affiliation: GPRD, Abbott Laboratories, Abbott Park, IL 60064-6123, USA. chen.zhao@abbott.com
authors.forename: Chen
authors.initials: C
authors.lastname: Zhao
authors.forename: Hing L
authors.initials: HL
authors.lastname: Sham
authors.forename: Minghua
authors.initials: M
authors.lastname: Sun
authors.forename: Vincent S
authors.initials: VS
authors.lastname: Stoll
authors.forename: Kent D
authors.initials: KD
authors.lastname: Stewart
authors.forename: Shuqun
authors.initials: S
authors.lastname: Lin
authors.forename: Hongmei
authors.initials: H
authors.lastname: Mo
authors.forename: Sudthida
authors.initials: S
authors.lastname: Vasavanonda
authors.forename: Ayda
authors.initials: A
authors.lastname: Saldivar
authors.forename: Chang
authors.initials: C
authors.lastname: Park
authors.forename: Edith J
authors.initials: EJ
authors.lastname: McDonald
authors.forename: Kennan C
authors.initials: KC
authors.lastname: Marsh
authors.forename: Larry L
authors.initials: LL
authors.lastname: Klein
authors.forename: Dale J
authors.initials: DJ
authors.lastname: Kempf
authors.forename: Daniel W
authors.initials: DW
authors.lastname: Norbeck
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D018432:Drug Resistance, Multiple; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000627:therapeutic use; D015497:HIV-1 / Q000187:drug effects*; D008024:Ligands; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D019438:Ritonavir / Q000138:chemical synthesis / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D001372:Aza Compounds; D017320:HIV Protease Inhibitors; D008024:Ligands; D014508:Urea; D019438:Ritonavir