title: Novel azacyclic ureas that are potent inhibitors of HIV-1 protease.
abstract: A series of novel, azacyclic ureas which are highly potent inhibitors of the HIV-1 protease (IC50 = 4.1 to < 0.5 nM) were synthesized. Aqueous solubilities of this series of compounds were improved by incorporating polar functional groups at the P1' P2 and P2' positions. These compounds also possess good anti-viral activity by inhibition of the cytopathic effect of HIV-13B in MT-4 cells in vitro.
authors: Abbott Laboratories, Abbott Park, Illinois 60064-3500, USA.
authors: H L
authors: HL
authors: Sham
authors: C
authors: C
authors: Zhao
authors: K C
authors: KC
authors: Marsh
authors: D A
authors: DA
authors: Betebenner
authors: S
authors: S
authors: Lin
authors: W
authors: W
authors: Rosenbrook
authors: T
authors: T
authors: Herrin
authors: L
authors: L
authors: Li
authors: D
authors: D
authors: Madigan
authors: S
authors: S
authors: Vasavanonda
authors: A
authors: A
authors: Molla
authors: A
authors: A
authors: Saldivar
authors: E
authors: E
authors: McDonald
authors: N E
authors: NE
authors: Wideburg
authors: D
authors: D
authors: Kempf
authors: D W
authors: DW
authors: Norbeck
authors: J J
authors: JJ
authors: Plattner
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001682:Biological Availability; D002460:Cell Line; D016333:HIV Protease / Q000235:genetics; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D008297:Male; D008969:Molecular Sequence Data; D051381:Rats; D017207:Rats, Sprague-Dawley; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000235:genetics; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D017320:HIV Protease Inhibitors; D011994:Recombinant Proteins; D014508:Urea; D016333:HIV Protease