Synthesis of potent and orally active HIV-protease inhibitors.
A series of potent HIV-protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma even after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially suitable for large scale production was developed.
Capraro
H G
HG
Ciba-Geigy Ltd., Basel, Switzerland.
Bold
G
G
Fässler
A
A
Cozens
R
R
Klimkait
T
T
Lazdins
J
J
Mestan
J
J
Poncioni
B
B
Rösel
J L
JL
Stover
D
D
Lang
M
M
D000284:Administration, Oral; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D000092502:Renin Inhibitors
D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D017320:HIV Protease Inhibitors; D000092502:Renin Inhibitors