Synthesis and evaluations of GLP-1 secretion and anti-diabetic effect in KKAy mice of new tricyclic compounds

Daisuke Minehira, Daisuke Takeda, Shota Miyawaki, Atsushi Kato, Isao Adachi, Akira Miyazaki, Ryuta Miyatake, Masahito Umezaki, Kyoko Miura, Yoshiro Kitahara, Kenji Sugimoto, Yuji Matsuya, Naoki Toyooka*

*この論文の責任著者

研究成果: ジャーナルへの寄稿学術論文査読

1 被引用数 (Scopus)

抄録

Glucagon-like peptide-1 (GLP-1), which belongs to the family of incretins, plays important role for the regulation of plasma glucose. Accordingly, GLP-1-based therapies for type 2 diabetes have recognized as one of the most interesting target. In this study, we have found the new tricyclic compounds having strong GLP-1 secretion from human intestinal L cells, and anti-diabetic properties in spontaneously obese and diabetic KKAy mice. The most potent compound 5ka was obtained as the unexpected product, and we would like to report the details of the synthesis, structure elucidations, pharmacological activities on secretion of GLP-1, and anti-diabetic effects using diabetic KKAy mice.

本文言語英語
ページ(範囲)372-404
ページ数33
ジャーナルHeterocycles
90
1
DOI
出版ステータス出版済み - 2015

ASJC Scopus 主題領域

  • 分析化学
  • 薬理学
  • 有機化学

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