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

Bioorg Med Chem Lett

Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.

Published: June 2006

AI Article Synopsis

  • Researchers developed new PPARdelta agonists based on the structure of GW2433, a non-selective ligand.
  • One compound, referred to as Compound 1, is effective at a concentration of 10 nM and is bioavailable.
  • Importantly, Compound 1 does not interact with other PPAR subtypes even at concentrations up to 10 microM, making it valuable for studying the effects of selectively activating PPARdelta.

Article 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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http://dx.doi.org/10.1016/j.bmcl.2006.02.079DOI Listing

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