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  • Title: Studies towards the conception of new selective PPARbeta/delta ligands.
    Author: Basséne CE, Suzenet F, Hennuyer N, Staels B, Caignard DH, Dacquet C, Renard P, Guillaumet G.
    Journal: Bioorg Med Chem Lett; 2006 Sep 01; 16(17):4528-32. PubMed ID: 16797985.
    Abstract:
    In order to define new PPARbeta/delta ligands, SAR study on the selective PPARbeta/delta activator L-165,041 led to the identification of one key functional group for selective PPARbeta/delta activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARbeta/delta subtype selectivity.
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