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

doi:10.3987/COM-14-S(K)29

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^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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Abstract

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.

Original language	English
Pages (from-to)	372-404
Number of pages	33
Journal	Heterocycles
Volume	90
Issue number	1
DOIs	https://doi.org/10.3987/COM-14-S(K)29
State	Published - 2015

ASJC Scopus subject areas

Analytical Chemistry
Pharmacology
Organic Chemistry

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3987/COM-14-S(K)29

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

abstract = "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.",

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

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year = "2015",

doi = "10.3987/COM-14-S(K)29",

language = "英語",

volume = "90",

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T1 - Synthesis and evaluations of GLP-1 secretion and anti-diabetic effect in KKAy mice of new tricyclic compounds

AU - Minehira, Daisuke

AU - Takeda, Daisuke

AU - Miyawaki, Shota

AU - Kato, Atsushi

AU - Adachi, Isao

AU - Miyazaki, Akira

AU - Miyatake, Ryuta

AU - Umezaki, Masahito

AU - Miura, Kyoko

AU - Kitahara, Yoshiro

AU - Sugimoto, Kenji

AU - Matsuya, Yuji

AU - Toyooka, Naoki

PY - 2015

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N2 - 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.

AB - 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.

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SN - 0385-5414

VL - 90

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JF - Heterocycles

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ER -

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

Abstract

ASJC Scopus subject areas

UN SDGs

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