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Issue 30, 2012
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Synthesis and evaluation of new polyenic compounds as potential PPARs modulators

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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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Supplementary files

Article information


Submitted
21 Mar 2012
Accepted
02 Apr 2012
First published
03 Apr 2012

Org. Biomol. Chem., 2012,10, 6169-6185
Article type
Paper

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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