Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity

被引：14
|
作者：
Motoshima, Kazunori [1 ]
Ishikawa, Minoru [1 ]
Hashimoto, Yuichi [1 ]
Sugita, Kazuyuki [1 ]
机构：
[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 10期
基金：
日本学术振兴会;
关键词：
PPAR agonist; Molecular design; Nuclear receptor; Subtype selectivity; ALPHA-GLUCOSIDASE INHIBITORS; PHENYLGLYCINE METHYL-ESTER; STRUCTURAL DEVELOPMENT; CARBOXYLIC-ACIDS; NUCLEAR RECEPTOR; PHTHALIMIDE SKELETON; METABOLIC SYNDROME; PPAR-DELTA; EVOLUTION; DESIGN;
D O I：
10.1016/j.bmc.2011.03.065
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3156 / 3172
页数：17
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