Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.

作者信息

Brooks D A, Etgen G J, Rito C J, Shuker A J, Dominianni S J, Warshawsky A M, Ardecky R, Paterniti J R, Tyhonas J, Karanewsky D S, Kauffman R F, Broderick C L, Oldham B A, Montrose-Rafizadeh C, Winneroski L L, Faul M M, McCarthy J R

机构信息

Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.

出版信息

J Med Chem. 2001 Jun 21;44(13):2061-4. doi: 10.1021/jm0155188.

Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARgamma- and PPARalpha-selective compounds, exhibits potent dual PPARalpha/gamma agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lowering and lipid/cholesterol homeostasis.