Potent HIV-1 protease inhibitors with antiviral activities in vitro.
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.
Sham
H L
HL
Abbott Laboratories, Pharmaceutical Discovery Division, Illinois 60064-3500.
Betebenner
D A
DA
Wideburg
N E
NE
Saldivar
A C
AC
Kohlbrenner
W E
WE
Vasavanonda
S
S
Kempf
D J
DJ
Norbeck
D W
DW
Zhao
C
C
Clement
J J
JJ
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
D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D007659:Ketones; D011480:Protease Inhibitors; D011994:Recombinant Proteins