1. 1,3,5-Trisubstituted Aryls as Highly Selective PPARδ Agonists
- Author
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Badry Bursulaya, Robert Epple, Andrea Gerken, Shin-Shay Tian, Mihai Azimioara, Maya Iskandar, and Ross Russo
- Subjects
Models, Molecular ,Agonist ,Molecular model ,medicine.drug_class ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Peroxisome proliferator-activated receptor ,Ligands ,Biochemistry ,Chemical synthesis ,PPAR agonist ,Structure-Activity Relationship ,Drug Discovery ,medicine ,PPAR delta ,Molecular Biology ,chemistry.chemical_classification ,Molecular Structure ,Chemistry ,Phenylurea Compounds ,Organic Chemistry ,General Medicine ,Highly selective ,Ligand (biochemistry) ,Butyrates ,Nuclear receptor ,Molecular Medicine ,Peroxisome proliferator-activated receptor delta - Abstract
A series of highly potent and selective PPARdelta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 microM, making it a useful tool in studying the biological effects of selective PPARdelta activation.
- Published
- 2006
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