Synthesis and biological evaluation of novel propylamine derivatives as orally active squalene synthase inhibitors
T Ishihara, H Kakuta, H Moritani, T Ugawa… - Bioorganic & medicinal …, 2004 - Elsevier
T Ishihara, H Kakuta, H Moritani, T Ugawa, I Yanagisawa
Bioorganic & medicinal chemistry, 2004•ElsevierSqualene synthase inhibitors are potentially superior hypolipidemic agents. We synthesized
novel propylamine derivatives, as well as evaluated their ability to inhibit squalene synthase
and their lipid-lowering effects in rats. 1-Allyl-2-[3-(benzylamino) propoxy]-9H-carbazole (YM-
75440) demonstrated potent inhibition of the enzyme derived from HepG2 cells with an IC50
value of 63nM. It significantly reduced both plasma total cholesterol and plasma triglyceride
levels following oral dosing to rats with a reduced tendency to elevate plasma transaminase …
novel propylamine derivatives, as well as evaluated their ability to inhibit squalene synthase
and their lipid-lowering effects in rats. 1-Allyl-2-[3-(benzylamino) propoxy]-9H-carbazole (YM-
75440) demonstrated potent inhibition of the enzyme derived from HepG2 cells with an IC50
value of 63nM. It significantly reduced both plasma total cholesterol and plasma triglyceride
levels following oral dosing to rats with a reduced tendency to elevate plasma transaminase …
Squalene synthase inhibitors are potentially superior hypolipidemic agents. We synthesized novel propylamine derivatives, as well as evaluated their ability to inhibit squalene synthase and their lipid-lowering effects in rats. 1-Allyl-2-[3-(benzylamino)propoxy]-9H-carbazole (YM-75440) demonstrated potent inhibition of the enzyme derived from HepG2 cells with an IC50 value of 63nM. It significantly reduced both plasma total cholesterol and plasma triglyceride levels following oral dosing to rats with a reduced tendency to elevate plasma transaminase levels.
Elsevier