Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene
Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene
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DOI：
10.1016/j.bmcl.2010.12.089
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发表时间：
2011-02-15
影响因子：
2.7
通讯作者：
Wisely, G. Bruce
中科院分区：
文献类型：
--
作者：
Bass, Jonathan Y.;Caravella, Justin A.;Wisely, G. Bruce
为了改善GSK 8062 1b的药物性质，制备了一系列杂芳基双环萘取代物。喹啉1c是一种等效的FXR激动剂，相对于1b具有改善的药物开发参数。此外，类似物1c在糖尿病DIO小鼠模型中降低体重增加和血清葡萄糖。(C)2010爱思唯尔有限公司版权所有。
To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes. (C) 2010 Elsevier Ltd. All rights reserved.