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Synthesis and the Intestinal Glucosidase Inhibitory Activity of 2-Aminoresorcinol Derivatives toward an Investigation of Its Binding Site

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Title: Synthesis and the Intestinal Glucosidase Inhibitory Activity of 2-Aminoresorcinol Derivatives toward an Investigation of Its Binding Site
Authors: KATO, Eisuke Browse this author →KAKEN DB
OIKAWA, Kenichi Browse this author
TAKAHASHI, Keisuke Browse this author
KAWABATA, Jun Browse this author →KAKEN DB
Keywords: glucosidase inhibitor
uncompetitive inhibition
diabetes mellitus
structure-activity relationship
Issue Date: May-2012
Publisher: 日本農芸化学会
Journal Title: Bioscience, Biotechnology, and Biochemistry
Volume: 76
Issue: 5
Start Page: 1044
End Page: 1046
Publisher DOI: 10.1271/bbb.120009
PMID: 22738986
Abstract: 2-Aminoresorcinol is a potent and selective intestinal glucosidase inhibitor. Unlike the majority of glucosidase inhibitors, it shows an uncompetitive mode of inhibition. In this study, we tested the intestinal glucosidase inhibitory activity of various 2-aminoresorcinol derivatives. We found that structural changes, in amino and two phenolic hydroxyl groups had a negative impact on inhibitory activity, but methylation of the phenolic hydroxyl group was found to maintain its activity and replacement of the aromatic ring with an acyl or alkoxy carbonyl group at the 4th position also retained its activity. This enable us to design a molecular probe for further study of the inhibition mechanism of 2-aminoresorcinol.
Type: article
URI: http://hdl.handle.net/2115/53431
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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