2. Academic Validation
  3. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity

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

  • Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21. doi: 10.1016/s0960-894x(03)00207-5.
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

Affiliation

  • 1 GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
PMID: 12699745 DOI: 10.1016/s0960-894x(03)00207-5
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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