Design and synthesis of a novel series of HIV-1 protease inhibitors.
The synthesis and the SAR study of novel pseudo symmetric inhibitors of HIV-1 protease are described. Michael addition of amino acid derivatives to vinyl ketones was utilized to derive a potent (nM) series of HIV-1 protease inhibitors.
Takashiro
E
E
Exploratory Chemistry Research Laboratories, Sankyo Co. Ltd., Tokyo, Japan.
Nakamura
Y
Y
Miyamoto
S
S
Ozawa
Y
Y
Sugiyama
A
A
Fujimoto
K
K
D015195:Drug Design; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
D017320:HIV Protease Inhibitors