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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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Publication details

The article was received on 21 Mar 2012, accepted on 02 Apr 2012 and first published on 03 Apr 2012


Article type: Paper
DOI: 10.1039/C2OB25593F
Citation: 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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