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

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Title: Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives
Authors: Kato, Eisuke Browse this author →KAKEN DB
Chikahisa, Fumiaki Browse this author
Kawabata, Jun Browse this author
Keywords: Pancreatic α-amylase
α-amylase inhibitor
diabetes mellitus
Issue Date: 23-Mar-2016
Journal Title: Tetrahedron Letters
Volume: 57
Issue: 12
Start Page: 1365
End Page: 1367
Publisher DOI: 10.1016/j.tetlet.2016.02.053
Abstract: 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.
Rights: © [2016]. This manuscript version is made available under the CC-BY-NC-ND 4.0 license
Type: article (author version)
Appears in Collections:農学院・農学研究院 (Graduate School of Agriculture / Faculty of Agriculture) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 加藤 英介

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