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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
CardarinePeroxisome proliferator-activated receptor alphaEC 50 (nM)3900N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor deltaEC 50 (nM)8N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)300N/AN/ADetails