Synthesis and structure-activity relationship of novel RXR antagonists: Orally active anti-diabetic and anti-obesity agents

被引：24

作者：

Sakaki, Junichi ^{[1
]}

Kishida, Masashi ^{[1
]}

Konishi, Kazuhide ^{[1
]}

Gunji, Hiroki ^{[1
]}

Toyao, Atsushi ^{[1
]}

Matsumoto, Yuki ^{[1
]}

Kanazawa, Takanori ^{[1
]}

Uchlyama, Hidefumi ^{[1
]}

Fukaya, Hiroaki ^{[1
]}

Mitani, Hironobu ^{[1
]}

Arai, Yoshie ^{[1
]}

Kimura, Masaaki ^{[1
]}

机构：

[1] Tsukuba Res Inst, Novartis Inst Biomed Res, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 17期

关键词：

RXR; antagonist; anti-diabetic; anti-obesity;

D O I：

10.1016/j.bmcl.2007.06.080

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of diazepinylbenzoic acid derivatives were synthesized and tested in the inhibition assay of the transactivation of RXR. Oral treatment of cyano derivatives (16f) was found to show anti-diabetic and anti-obesity effects in KK-A(y) mice. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4804 / 4807

页数：4

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