Design, synthesis and metabolic regulation effect of farnesoid X receptor (FXR) antagonistic benzoxepin-5-ones

被引：1
|
作者：
Guo-Ning Zhang [1 ,2 ]
Yi Huan [1 ]
Xing Wang [1 ]
Su-Juan Sun [1 ]
Zhu-Fang Shen [1 ]
Wei-Shuo Fang [1 ]
机构：
[1] State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College
[2] Institute of Medicinal Biotechnology, Chinese Academy of Medical Science, Peking Union Medical College
来源：
ChineseChemicalLetters | 2017年 / 28卷 / 07期
关键词：
Farnesoid X receptor; Antagonist; Benzoxepin-5-one; Triglyceride; Plasma ALT;
D O I：
暂无
中图分类号：
TQ460.1 [基础理论];
学科分类号：
1007 ;
摘要：
A series of benzoxepin-5-ones were designed and synthesized by the cyclization of chalcones which were previously found as FXR antagonists. The cellular FXR antagonism of benzoxepines was investigated,among which the most potent compound 10 l was able to reduce the plasma and hepatic triglyceride and plasma ALT levels in mice.
引用
收藏
页码：1519 / 1522
页数：4
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