具有苯乙基苯酞骨架的过氧化物酶体增殖物激活受体激动剂来源于沙利度胺相关的肝 X 受体拮抗剂：绝对构型与亚型选择性的关系。
Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: relationship between absolute configuration and subtype selectivity.
机构信息
Institute of Molecular & Cellular Bioscience, The University of Tokyo, Yayoi, Bunkyo-ku, Japan.
出版信息
Bioorg Med Chem. 2011 May 15;19(10):3156-72. doi: 10.1016/j.bmc.2011.03.065. Epub 2011 Apr 3.
Introduction of an alkylcarboxylic acid unit, which is a partial structure of endogenous peroxisome proliferator-activated receptor (PPAR) ligands, into a phenethylphenylphthalimide skeleton, which possesses liver X receptor (LXR) antagonistic activity, afforded novel PPAR ligands. The results of structure-activity relationship analysis and docking studies led us to the potent PPAR agonists 13c-e. The absolute configuration of 13c-e affects the PPAR subtype selectivity.
将内源性过氧化物酶体增殖物激活受体 (PPAR) 配体的部分结构烷基羧酸单元引入具有肝 X 受体 (LXR) 拮抗活性的苯乙基苯酞酰亚胺骨架中，得到了新型的 PPAR 配体。构效关系分析和对接研究的结果导致了我们得到了有效的 PPAR 激动剂 13c-e。13c-e 的绝对构型影响 PPAR 亚型选择性。
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