Design, Synthesis, and Structural Analysis of Phenylpropanoic Acid-Type PPAR纬-Selective Agonists: Discovery of Reversed Stereochemistry鈭扐ctivity Relationship
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- 作者：Masao Ohashi ; Takuji Oyama ; Izumi Nakagome ; Mayumi Satoh ; Yoshino Nishio ; Hiromi Nobusada ; Shuichi Hirono ; Kosuke Morikawa ; Yuichi Hashimoto ; Hiroyuki Miyachi
- 刊名：Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：January 13, 2011
- 年：2011
- 卷：54
- 期：1
- 页码：331-341
- 全文大小：1178K
- 年卷期：v.54,no.1(January 13, 2011)
- ISSN：1520-4804
文摘
Peroxisome proliferator-activated receptor gamma (PPAR纬) is a ligand-mediated transcription factor with roles in glucose, lipid, and lipoprotein homeostasis, and PPAR纬 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 伪-benzylphenylpropanoic acid PPAR纬 agonists. Interestingly, these compounds show a reversal of the stereochemistry鈭抰ransactivation activity relationship observed with other phenylpropanoic acid ligands.