Issue 30, 2012
From the journal:

Organic & Biomolecular Chemistry

Synthesis and evaluation of new polyenic compounds as potential PPARs modulators†‡

Dominique Amans,a   Véronique Bellosta,a   Catherine Dacquet,*b   Alain Ktorza,b   Nathalie Hennuyer,cde   Bart Staels,cde   Daniel-Henri Caignard*f  and  Janine Cossy*a  

* Corresponding authors

a Laboratoire de Chimie Organique, ESPCI Paris Tech, CNRS, 10 rue Vauquelin, 75231-PARIS Cedex 05, France
E-mail: janine.cossy@espci.fr

b Division of Metabolic Disease Research, Institut de Recherches Servier, 11 Rue des Moulineaux, 92150 Suresnes, France

c Université Lille Nord de France, Lille, France

d Inserm, U1011, Lille, France

e Institut Pasteur de Lille, F-59019 Lille, France

f Experimental Science Division Institut de Recherches Servier, 11 Rue des Moulineaux, 92150 Suresnes, France

Abstract

In order to identify new leads for the treatment of type 2 diabetes, polyenic molecules A and B derived from nipecotic acid and dienol derivatives C have been prepared and their effect on PPARs transcriptional activity evaluated and compared to that of rosiglitazone, WY14,643 and GW501516. Among the synthesized compounds, dienol 39 is the most active, increasing WY14,643 PPARα response and demonstrating partial agonist properties on rosiglitazone PPARγ.

Graphical abstract: Synthesis and evaluation of new polyenic compounds as potential PPARs modulators

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Article information

DOI
https://doi.org/10.1039/C2OB25593F
Article type
Paper
Submitted
21 Mar 2012
Accepted
02 Apr 2012
First published
03 Apr 2012

Org. Biomol. Chem., 2012,10, 6169-6185

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Synthesis and evaluation of new polyenic compounds as potential PPARs modulators

D. Amans, V. Bellosta, C. Dacquet, A. Ktorza, N. Hennuyer, B. Staels, D. Caignard and J. Cossy, Org. Biomol. Chem., 2012, 10, 6169 DOI: 10.1039/C2OB25593F

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