Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor

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

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Natural product acyl-CoA:cholesterol acyltrasferase (ACAT) inhibitor pyripyropene A was synthetically converted to acetylcholinesterase (AChE) inhibitor via heterolitic cleavage of the 2-pyrone ring, followed by γ-acylation/cyclization with several aroyl chlorides. The 4-pyridyl analogue selectively showed AChE inhibitory activity (IC50 = 7.9 μM) and no ACAT inhibitory activity IC50 = > 1000 μM. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1315-1316
Number of pages2
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number12
DOIs
Publication statusPublished - 2000 Jun 19

ASJC Scopus subject areas

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

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  • Cite this

    Obata, R., Sunazuka, T., Otoguro, K., Tomoda, H., Harigaya, Y., & Omura, S. (2000). Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor. Bioorganic and Medicinal Chemistry Letters, 10(12), 1315-1316. https://doi.org/10.1016/S0960-894X(00)00218-3