Role of the thiosugar ring in the inhibitory activity of salacinol, a potent natural α-glucosidase inhibitor

Author:

Takashima Katsuki1ORCID,Nakamura Shinya1,Nagayama Maiko1,Marumoto Shinsuke2,Ishikawa Fumihiro1ORCID,Xie Weijia3ORCID,Nakanishi Isao1,Muraoka Osamu4,Morikawa Toshio4ORCID,Tanabe Genzoh14ORCID

Affiliation:

1. Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan

2. Joint Research Centre, Kindai University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan

3. State Key Laboratory of Natural Medicines, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 2100009, P. R. China

4. Pharmaceutical Research and Technology Institute, Kindai University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan

Abstract

In contrast to previous SAR studies of aza-compounds (23vs.24 and 25), the present study using analogues (26a–26c, 27c, and 28a–28c) of salacinol (1) revealed an essential role of the thiosugar ring in effectively inhibiting α-glucosidase.

Funder

Japan Society for the Promotion of Science London

Mochida Memorial Foundation for Medical and Pharmaceutical Research

Publisher

Royal Society of Chemistry (RSC)

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