Phenoxyacetic acids as PPARδ partial agonists: Synthesis, optimization, and in vivo efficacy

Karen A. Evans, Barry G. Shearer, David D. Wisnoski, Dongchuan Shi, Steven M. Sparks, Daniel D. Sternbach, Deborah A. Winegar, Andrew N. Billin, Christy Britt, James M. Way, Andrea H. Epperly, Lisa M. Leesnitzer, Raymond V. Merrihew, Robert X. Xu, Millard H. Lambert, Jian Jin

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

A series of phenoxyacetic acids as subtype selective and potent hPPARδ partial agonists is described. Many analogues were readily accessible via a single solution-phase synthetic route which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of two potent exemplars which were further evaluated in vivo. Details of the SAR, optimization, and in vivo efficacy of this series are presented herein.

Original languageEnglish
Pages (from-to)2345-2350
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number8
DOIs
StatePublished - 15 Apr 2011
Externally publishedYes

Keywords

  • PPARd
  • Partial agonist

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