Co-crystal structure guided array synthesis of PPARγ inverse agonists

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 o...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (14), p.3916-3920
Main Authors: Trump, Ryan P., Cobb, Jeffrey E., Shearer, Barry G., Lambert, Millard H., Nolte, Robert T., Willson, Timothy M., Buckholz, Richard G., Zhao, Sumin M., Leesnitzer, Lisa M., Iannone, Marie A., Pearce, Kenneth H., Billin, Andrew N., Hoekstra, William J.
Format: Article
Language:English
Subjects:
Biological and medical sciences
General and cellular metabolism. Vitamins
Inverse agonist
Medical sciences
Pharmacology. Drug treatments
PPARγ
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.111