Peroxizome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists : relationship between absolute configuration and subtype selectivity
Peroxizome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists : relationship between absolute configuration and subtype selectivity
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具有源自沙利度胺相关肝脏 X 受体拮抗剂的苯乙基苯基邻苯二甲酰亚胺骨架的过氧化物酶增殖物激活受体激动剂：绝对构型与亚型选择性之间的关系
DOI：
10.1016/j.bmc.2011.03.065
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
K.Sugita
中科院分区：
文献类型：
--
作者：
K.Motoshima;M.Ishikawa;Y.Hashimoto;K.Sugita
引入一个烷基羧酸单元，这是一个部分结构的内源性过氧化物酶体增殖物激活受体（PPAR）配体，到苯乙基苯基邻苯二甲酰亚胺骨架，它具有肝X受体（LXR）拮抗活性，提供了新的PPAR配体。构效关系分析和对接研究的结果使我们找到了有效的PPAR激动剂13 c-e。13 c-ε的绝对构型影响了PPAR亚型的选择性。
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 agonists13c–e. The absolute configuration of13c–eaffects the PPAR subtype selectivity.