Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor α/δ dual agonists

Jun Ichi Kasuga, Makoto Makishima, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

36 Citations (Scopus)

Abstract

A series of phenylpropanoic acids was prepared as candidate dual agonists of peroxisome proliferator-activated receptors (PPAR) α and δ. Structure-activity relationship studies indicated that the shape of the linker moiety and the nature of the substituent at the distal benzene ring play key roles in determining the potency and selectivity of PPAR subtype transactivation. Optically active α-ethylphenylpropanoic acid derivatives were identified as potent human PPAR α and δ dual agonists with potential for the treatment of metabolic syndrome.

Original languageEnglish
Pages (from-to)554-558
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number3
DOIs
Publication statusPublished - Feb 1 2006

Keywords

  • Metabolic syndrome
  • PPAR
  • PPARα
  • PPARδ

ASJC Scopus subject areas

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

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