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International Research Journal of Pure and Applied Chemistry

International Research Journal of Pure and Applied Chemistry, ISSN: 2231-3443,Vol.: 14, Issue.: 2

Short Research Article

Simple Synthesis of Sulfonyl Amidine-Containing Glucosidase Inhibitors by a Chemoselective Coupling Reaction Between D-Gluconothiolactam and Sulfonyl Azides


Muhammad Aswad1,2, Junya Chiba1*, Takenori Tomohiro1 and Yasumaru Hatanaka1

1Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.

2Faculty of Pharmacy, Hasanuddin University, Makassar, South Sulawesi 90245, Indonesia.


Article Information


(1) Richard Sawadogo, Postdoc, Group Cell death & Natural Compounds Laboratoire de Biologie Moléculaire et Cellulaire du Cancer Hôpital Kirchberg, Luxembourg.


(1) Xionghao Lin, Howard University, United States of America.

(2) Mohini Chetan Kuchekar, Pune University, India.

Complete Peer review History: http://www.sciencedomain.org/review-history/19549




In this report, we describe a simple synthesis of gluconoamidinylsulfones as a new class of potential inhibitors toward glycan processing enzymes. Gluconoamidinylsulfones have a glucose-based sulfonyl amidine skeleton, thus would form a distorted half-chair conformation with positive charge, which is analogous to transition state in the enzymatic process. A chemoselective coupling reaction between thioamide and sulfonyl azide enabled one-step synthesis of the iminosugar derivatives from commercially available D-gluconothiolactam in a protection-free manner. The phenyl-substituted gluconoamidinylsulfone displayed high inhibitory ability toward α- and β-glucosidases with Ki values of 13.9 and 8.2 μM, respectively, resulting that gluconoamidinylsulfones would be expected to entry in a new class of promising potential inhibitors toward various glycan-processing enzymes.


Keywords :

Inhibitor; glycosidase; iminosugar; coupling reaction; one-step synthesis; thioamide; sulfonyl azide; gluconoamidinylsulfone.


Full Article - PDF    Page 1-8    Article Metrics


DOI : 10.9734/IRJPAC/2017/34259

Review History    Comments

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