Pseudo-symmetrical difluoroketones. Highly potent and specific inhibitors of HIV-1 protease.
A series of novel, pseudo-symmetrical difluoroketones which are highly potent inhibitors of the HIV-1 protease (IC50 = 1.55-0.02 nM) were synthesized. These compounds also possess good antiviral activity by inhibition of the cytopathic effect of HIV-13B in MT-4 cells in vitro.
Sham
H L
HL
Abbott Laboratories, Abbott Park, IL 60064-3500.
Betebenner
D A
DA
Wideburg
N
N
Saldivar
A C
AC
Kohlbrenner
W E
WE
Craig-Kennard
A
A
Vasavanonda
S
S
Kempf
D J
DJ
Clement
J J
JJ
Erickson
J E
JE
D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D017320:HIV Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D007659:Ketones; D011994:Recombinant Proteins