Title of article :
Design, synthesis, and structure–activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonists
Author/Authors :
Nam-Jung Kim، نويسنده , , Kwang-Ok Lee، نويسنده , , Bon-Woong Koo، نويسنده , , Funan Li، نويسنده , , Ja-Kyung Yoo، نويسنده , , Hyun Ju Park، نويسنده , , Kyung-Hoon Min، نويسنده , , Joong-Yeon Lim، نويسنده , , Mi Kyung Kim، نويسنده , , Jin-Kwan Kim، نويسنده , , Young-Ger Suh، نويسنده ,
Abstract :
We have developed a new class of PPARα/γ dual agonists, which show excellent agonistic activity in PPARα/γ transactivation assay. In particular, (R)-9d was identified as a potent PPARα/γ dual agonist with EC50s of 0.377 μM in PPARα and 0.136 μM in PPARγ, respectively. Interestingly, the structure–activity relationship revealed that the stereochemistry of the identified PPARα/γ dual agonists significantly affects their agonistic activities in PPARα than in PPARγ.
