- A Short and Efficient Synthesis of the Pharmacological Research Tool GW501516 for the Peroxisome Proliferator-Activated Receptor δ
-
The most potent and selective peroxisome proliferator-activated receptor δ (PPARδ) agonist GW501516 (1) was synthesized in 4 steps and 78% overall yield starting from o-cresol by using a one-pot regiocontrolled dialkylation of mercaptophenol 5 as the key
- Wei, Zhi-Liang,Kozikowski, Alan P.
-
-
Read Online
- Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogs
-
Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARβ/δ agonist yet described, and equally selective analogs at the thiazole-
- Pereira, Raquel,Gaudon, Claudine,Iglesias, Beatriz,Germain, Pierre,Gronemeyer, Hinrich,De Lera, Angel R.
-
-
- Activator of PPAR delta
-
Compounds of Formula (I) are disclosed. These compounds include selective activators of human PPAR delta.
- -
-
-
- Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity
-
We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor δ (PPARδ). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC50 of 1.1 nM against PPARδ with 1000-fold selectivity over the other human subtypes.
- Sznaidman, Marcos L.,Haffner, Curt D.,Maloney, Patrick R.,Fivush, Adam,Chao, Esther,Goreham, Donna,Sierra, Michael L.,LeGrumelec, Christelle,Xu, H. Eric,Montana, Valerie G.,Lambert, Millard H.,Willson, Timothy M.,Oliver Jr., William R.,Sternbach, Daniel D.
-
p. 1517 - 1521
(2007/10/03)
-