Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives

Kato, Eisuke; Chikahisa, Fumiaki; Kawabata, Jun

Tetrahedron Letters, 2016, 57(12), 1365-1367

Permalink : https://hdl.handle.net/2115/68675

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アクセス権
open access
URI
https://hdl.handle.net/2115/68675
タイトル
Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives
著者
Kato, Eisuke ; Chikahisa, Fumiaki ; Kawabata, Jun
e-Rad_Researcher
40466446
著者名
Kato, Eisuke
著者名
Chikahisa, Fumiaki
著者名
Kawabata, Jun
言語
英語
キーワード
Pancreatic　α-amylase
α-amylase inhibitor
diabetes mellitus
acarviosin
transglycosylation
発行日
2016-03-23
収録物名
Tetrahedron Letters
巻(号)
57(12)
ページ
1365-1367
抄録
Pancreatic α-amylase is a target for type 2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized conjugates of glucose and acarviosin. The synthetic compounds showed mild α-amylase inhibitory activity with higher activity compared with non-glucose conjugated compounds, but lower activity compared to acarviosin. Comparison of these activities revealed transglycosylation of acarviosin during the enzyme reaction. Additionally, the α-amylase inhibitory activity of acarviosin is expressed through these transglycosylation products.
資源タイプ
学術雑誌論文
出版タイプ
Accepted Manuscript
権利情報
Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International
権利情報
© [2016]. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
PISSN
0040-4039
関連情報 (isVersionOf)
出版社版DOI
https://doi.org/10.1016/j.tetlet.2016.02.053