title: Potent HIV-1 protease inhibitors with antiviral activities in vitro.
abstract: A series of novel difluoroketones with low molecular weight (less than 600 m.u.) and which are potent inhibitors of the HIV-1 protease (IC50 = 1.0 to 21 nM) were synthesized. These compounds also exhibited antiviral activity by inhibition of the cytopathic effect of HIV-1(3)B in MT-4 cells in vitro.
authors.affiliation: Abbott Laboratories, Pharmaceutical Discovery Division, Illinois 60064-3500.
authors.forename: H L
authors.initials: HL
authors.lastname: Sham
authors.forename: D A
authors.initials: DA
authors.lastname: Betebenner
authors.forename: N E
authors.initials: NE
authors.lastname: Wideburg
authors.forename: A C
authors.initials: AC
authors.lastname: Saldivar
authors.forename: W E
authors.initials: WE
authors.lastname: Kohlbrenner
authors.forename: S
authors.initials: S
authors.lastname: Vasavanonda
authors.forename: D J
authors.initials: DJ
authors.lastname: Kempf
authors.forename: D W
authors.initials: DW
authors.lastname: Norbeck
authors.forename: C
authors.initials: C
authors.lastname: Zhao
authors.forename: J J
authors.initials: JJ
authors.lastname: Clement
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D017320:HIV Protease Inhibitors; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D007659:Ketones; D011480:Protease Inhibitors; D011994:Recombinant Proteins