Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)

Rika Obata, Toshiaki Sunazuka, Hiroshi Tomoda, Yoshihiro Harigaya, Satoshi Omura

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

Modification and structure-activity relationships of ACAT inhibitor pyripyropene were examined. PR-109 (7g) showed the most potent (IC50 = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activity (IC50 = 19 nM) and its in vivo activity improved 10 times better (ED50 = 10 mg/kg) than that of pyripyropene A.

Original languageEnglish
Pages (from-to)2683-2688
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number22
DOIs
Publication statusPublished - 1995 Nov 16

ASJC Scopus subject areas

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

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