Synthesis and biological evaluation of a focused library of beauveriolides

Kenichiro Nagai, Takayuki Doi, Taichi Ohshiro, Toshiaki Sunazuka, Hiroshi Tomoda, Takashi Takahashi, Satoshi Omura

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Fungal beauveriolide III (1b), discovered as an inhibitor of lipid droplet accumulation in mouse macrophages and showing antiatherogenic activity in mouse model, consists of l-Phe, l-Ala, d-allo-Ile, and (3S, 4S)-3-hydroxy-4-methyloctanoic acid moieties. A combinatorial library of beauveriolide analogues focusing on l-Ala and d-allo-Ile of 1b was synthesized by combinatorial synthesis. Among them, d-Ala analogues consisting of A{2} improved their solubility, while those with 7{1, 3, 2},7{2, 3, 1}, and 7{2, 3, 2} were 20 times more potent than 1b.

Original languageEnglish
Pages (from-to)4397-4400
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number15
DOIs
Publication statusPublished - 2008 Aug 1
Externally publishedYes

Keywords

  • ACAT
  • Antiatherogenic activity
  • Cyclic depsipeptide
  • Focused library

ASJC Scopus subject areas

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

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