Bioorganic & Medicinal Chemistry Letters 2002-12-16

Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.

Markus Thor, Katarina Beierlein, Graeme Dykes, Anna Lena Gustavsson, Jessica Heidrich, Lena Jendeberg, Bengt Lindqvist, Cecile Pegurier, Patrick Roussel, Martin Slater, Stefan Svensson, Mona Sydow-Bäckman, Ulla Thornström, Jonas Uppenberg

Index: Bioorg. Med. Chem. Lett. 12(24) , 3565-7, (2002)

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Abstract

A series of 5-substituted 2-benzoylaminobenzoic acids has been synthesized and assayed for PPARalpha/gamma activity. Both dual activators and selective PPARgamma agonists have been identified. This class of compounds was shown to activate the PPARgamma receptor through interaction with a novel binding site.