Design, Synthesis, and Structural Analysis of Phenylpropanoic Acid-Type PPAR gamma-Selective Agonists Discovery of Reversed Stereochemistry-Activity Relationship

作者：Ohashi Masao; Oyama Takuji; Nakagome Izumi; Satoh Mayumi; Nishio Yoshino; Nobusada Hiromi; Hirono Shuichi; Morikawa Kosuke; Hashimoto Yuichi; Miyachi Hiroyuki^*

来源：Journal of Medicinal Chemistry, 2011, 54(1): 331-341.

DOI：10.1021/jm101233f

Peroxisome proliferator-activated receptor gamma (PPAR gamma) is a ligand-mediated transcription factor with roles in glucose, lipid, and lipoprotein homeostasis, and PPAR gamma ligands are expected have therapeutic potential in these as well as other areas We report here the design, synthesis, crystallographic analysis, and computational studies of alpha-benzylphenylpropanoic acid PPAR gamma agonists Interestingly, these compounds show a reversal of the stereochemistry-transactivation activity relationship observed with other phenylpropanoic acid ligands

• 出版日期2011-1-13
• 单位河北医科大学