Co-crystal structure guided array synthesis of PPARγ inverse agonists
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- 作者：Ryan P. Trump ; Jeffrey E. Cobb ; Barry G. Shearer ; Millard H. Lambert ; Robert T. Nolte ; Timothy M. Willson ; Richard G. Buckholz ; Sumin M. Zhao ; Lisa M. Leesnitzer ; Marie A. Iannone ; et al.
- 关键词：PPARγ ; Inverse agonist
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 July 2007
- 年：2007
- 卷：17
- 期：14
- 页码：3916-3920
- 全文大小：192 K
文摘
PPARγ-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARγ rich adipose. Both pro- and anti-adipogenic PPARγ ligands promote glucose and lipid lowering in animal models of diabetes. Herein, we disclose representatives of an array of 160 farglitazar analogues with atypical inverse agonism of PPARγ in mature adipocytes.