Studies towards the conception of new selective PPARbeta/delta ligands.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) {4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy}acetic acid Peroxisome proliferator-activated receptor delta EC 50 (nM) 125 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 10000 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 1 N/A N/A Details