Studies towards the conception of new selective PPARbeta/delta ligands.

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Bassene CE, Suzenet F, Hennuyer N, Staels B, Caignard DH, Dacquet C, Renard P, Guillaumet G

Studies towards the conception of new selective PPARbeta/delta ligands.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4528-32. Epub 2006 Jun 23.

PubMed ID
16797985 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
{4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy}acetic acidPeroxisome proliferator-activated receptor deltaEC 50 (nM)125N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor alphaEC 50 (nM)10000N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor deltaEC 50 (nM)1N/AN/ADetails