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

Autor: Trump RP; Drug Discovery, GlaxoSmithKline, Research Triangle Park, NC 27709, USA., Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jul 15; Vol. 17 (14), pp. 3916-20. Date of Electronic Publication: 2007 May 18.
DOI: 10.1016/j.bmcl.2007.04.111
Abstrakt: 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.
Databáze: MEDLINE