Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
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Havranek M, Sauerberg P, Mogensen JP, Kratina P, Jeppesen CB, Pettersson I, Pihera P
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4144-9. Epub 2007 May 21.
- PubMed ID
- 17553681 [ View in PubMed]
- Abstract
Y-shaped molecules bearing alkynylallylic moieties were found to be potent and selective PPARdelta activators. The alkynylallylic moiety was synthesized from alkyn-1-ols by hydroalumination followed by a cross-coupling reaction. Series of active compounds 6 were obtained by stepwise changing the structure of the known PPARpan agonist 5 into Y-shaped compounds. The most active and selective compound, 6f, had a PPARdelta potency of 0.13 microM, which is 50-fold more potent than compound 5.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 3900 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 8 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 300 N/A N/A Details