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Comparative Study
. 2003 May 5;13(9):1517-21.
doi: 10.1016/s0960-894x(03)00207-5.

Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity

Marcos L Sznaidman  1 , Curt D Haffner, Patrick R Maloney, Adam Fivush, Esther Chao, Donna Goreham, Michael L Sierra, Christelle LeGrumelec, H Eric Xu, Valerie G Montana, Millard H Lambert, Timothy M Willson, William R Oliver Jr, Daniel D Sternbach
Affiliations
Comparative Study

Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity

Marcos L Sznaidman et al. Bioorg Med Chem Lett. .

Abstract

We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor delta (PPARdelta). 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 EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes.

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