Synthesis of branched seven-membered 1-N-iminosugars and their evaluation as glycosidase inhibitors

被引:10
|
作者
Li, Hongqing [1 ]
Zhang, Yongmin [1 ]
Favre, Sylvain [2 ]
Vogel, Pierre [2 ]
Sollogoub, Matthieu [1 ]
Bleriot, Yves [1 ]
机构
[1] Univ Paris 06, Inst Parisien Chim Mol, CNRS, UMR 7201,FR 2769, F-75005 Paris, France
[2] Ecole Polytech Fed Lausanne, Inst Sci & Ingn Chim, BCH, CH-1015 Lausanne, Switzerland
关键词
Iminosugar; Glycosidase; Inhibitor; Azepane; TYPE-2; DIABETES-MELLITUS; THERAPEUTIC APPLICATIONS; ISOFAGOMINE; POTENT; AGENTS; GLUCOSIDASE; IMINOSUGARS; CATION; RING; TETRAHYDROXYAZEPANES;
D O I
10.1016/j.carres.2011.10.039
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Four branched tetra- and pentahydroxylated azepanes have been synthesized from a common azepane precursor through dihydroxylation followed by deoxygenation. They have been assayed as glycosidase inhibitors on a panel of 22 glycosidases and one methylated azepane displayed selective, competitive, and moderate inhibition toward bovine kidney alpha-L-fucosidase. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:110 / 114
页数:5
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