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[L-亚氨基呋喃糖的合成及其生物学评价]

[Synthesis of L-Iminofuranoses and Their Biological Evaluations].

作者信息

Natori Yoshihiro

机构信息

Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University.

出版信息

Yakugaku Zasshi. 2021;141(1):15-24. doi: 10.1248/yakushi.20-00194.

Abstract

Iminosugars are one of the compounds that mimic the structure of monosaccharides. Such sugar mimics have the ability to effectively and specifically inhibit various glycosidases and glycosyltransferases. After studying iminopyranose, miglitol, which has α-glucosidase inhibitory activity, was approved and used in the clinical treatment of diabetes. This study focused on l-iminofuranose derivatives to develop new anti-diabetic drug. As a result, it was found that l-iminofuranose having an alkyl group at C1 position show potent α-glucosidase inhibitory activity. Further structural-activity relationship studies were conducted, and interesting findings were obtained. This paper describes the details of those research developments.

摘要

亚氨基糖是一类模拟单糖结构的化合物。这类糖模拟物能够有效且特异性地抑制多种糖苷酶和糖基转移酶。在对亚氨基吡喃糖进行研究之后,具有α - 葡萄糖苷酶抑制活性的米格列醇被批准用于糖尿病的临床治疗。本研究聚焦于l - 亚氨基呋喃糖衍生物以开发新型抗糖尿病药物。结果发现,在C1位带有烷基的l - 亚氨基呋喃糖显示出强效的α - 葡萄糖苷酶抑制活性。进一步开展了构效关系研究,并获得了有趣的发现。本文描述了这些研究进展的详细情况。

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