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Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. Epub 2006 Mar 20.

1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.

Author information

1
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

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.

PMID:
16546385
DOI:
10.1016/j.bmcl.2006.02.079
[Indexed for MEDLINE]

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