1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists |
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| Authors: | Epple Robert Azimioara Mihai Russo Ross Bursulaya Badry Tian Shin-Shay Gerken Andrea Iskandar Maya |
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| Institution: | Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA. repple@gnf.org |
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| 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. |
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