Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ)—synthesis and biological activity
ML Sznaidman, CD Haffner, PR Maloney… - Bioorganic & medicinal …, 2003 - Elsevier
ML Sznaidman, CD Haffner, PR Maloney, A Fivush, E Chao, D Goreham, ML Sierra…
Bioorganic & medicinal chemistry letters, 2003•ElsevierWe 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.
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.
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.
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