Synthesis and biological evaluation of a focused library of beauveriolides

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

研究成果: Article査読

9 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)4397-4400
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
18
15
DOI
出版ステータスPublished - 2008 8 1
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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