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

30 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
Externally publishedYes

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Sterol O-Acyltransferase
Chemical modification
Structure-Activity Relationship
Inhibitory Concentration 50
pyripyropene A

ASJC Scopus subject areas

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

Cite this

Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA : Cholesterol O-acyltransferase (ACAT). / Obata, Rika; Sunazuka, Toshiaki; Tomoda, Hiroshi; Harigaya, Yoshihiro; Omura, Satoshi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 5, No. 22, 16.11.1995, p. 2683-2688.

Research output: Contribution to journalArticle

Obata, Rika ; Sunazuka, Toshiaki ; Tomoda, Hiroshi ; Harigaya, Yoshihiro ; Omura, Satoshi. / Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA : Cholesterol O-acyltransferase (ACAT). In: Bioorganic and Medicinal Chemistry Letters. 1995 ; Vol. 5, No. 22. pp. 2683-2688.
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