Author/Authors :
Eunkyung Kim، نويسنده , , Chan Sun Park، نويسنده , , Taedong Han، نويسنده , , Myung-Ho Bae، نويسنده , , Wonee Chong، نويسنده , , Choong Hyun Lee، نويسنده , , Young Ah Shin، نويسنده , , Byung-Nak Ahn، نويسنده , , Mi Kyung Kim، نويسنده , , Chang Yell Shin، نويسنده , , Moon Ho Son، نويسنده , , Jin-Kwan Kim، نويسنده , , Ho Sang Moon، نويسنده , , Hyun Joo Shim، نويسنده , , Eun Jung Kim، نويسنده , , Soon Hoe Kim، نويسنده , , Joong-Yeon Lim، نويسنده , , Chun Ho Lee، نويسنده ,
Abstract :
Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
Keywords :
Type 2 diabetes , PPARs , PPAR?/? dual agonists , tetrahydropyridine
