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Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18.

Co-crystal structure guided array synthesis of PPARgamma inverse agonists.

Author information

1
Drug Discovery, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.

Abstract

PPARgamma-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARgamma rich adipose. Both pro- and anti-adipogenic PPARgamma 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 PPARgamma in mature adipocytes.

PMID:
17533125
DOI:
10.1016/j.bmcl.2007.04.111
[Indexed for MEDLINE]

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