Issue 30, 2012

Synthesis and evaluation of new polyenic compounds as potential PPARs modulators

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

Supplementary files

Article information

Article type
Paper
Submitted
21 3 2012
Accepted
02 4 2012
First published
03 4 2012

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

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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