Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists

Jun ichi Kasuga, Seiichi Ishida, Daisuke Yamasaki, Makoto Makishima, Takefumi Doi, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

16 Citations (Scopus)


We designed and synthesized novel PPARδ antagonists based on the crystal structure of the PPARδ full agonist TIPP-204 bound to the PPARδ ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARδ-preferential antagonistic activity.

Original languageEnglish
Pages (from-to)6595-6599
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number23
Publication statusPublished - Dec 1 2009



  • Biphenylcarboxylic acid
  • PPAR
  • PPARδ
  • PPARδ antagonist

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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