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

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

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-12, Vol.12 (24), p.3565-3567
Main Authors: Thor, Markus, Beierlein, Katarina, Dykes, Graeme, Gustavsson, Anna-Lena, Heidrich, Jessica, Jendeberg, Lena, Lindqvist, Bengt, Pegurier, Cecile, Roussel, Patrick, Slater, Martin, Svensson, Stefan, Sydow-Bäckman, Mona, Thornström, Ulla, Uppenberg, Jonas
Format: Article
Language:English
Subjects:
Aminobenzoates - chemical synthesis
Aminobenzoates - pharmacology
Binding Sites
Biological and medical sciences
Crystallography, X-Ray
General and cellular metabolism. Vitamins
Humans
Medical sciences
Pharmacology. Drug treatments
Receptors, Cytoplasmic and Nuclear - agonists
Receptors, Cytoplasmic and Nuclear - genetics
Structure-Activity Relationship
Transcription Factors - agonists
Transcription Factors - genetics
Transcriptional Activation - drug effects
Transfection
Tumor Cells, Cultured
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Summary:A series of 5-substituted 2-benzoylaminobenzoic acids has been synthesized and assayed for PPARα/γ activity. Both dual activators and selective PPARγ agonists have been identified. This class of compounds was shown to activate the PPARγ receptor through interaction with a novel binding site. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00791-6