BETA-GLUCOSIDASE INHIBITORS INCORPORATING PYRIDINIUM AS A GLUCOSYL MIMIC

被引:7
作者
KNAPP, S [1 ]
DONG, YH [1 ]
RUPITZ, K [1 ]
WITHERS, SG [1 ]
机构
[1] UNIV BRITISH COLUMBIA,VANCOUVER,BC V6T 1Z1,CANADA
基金
加拿大自然科学与工程研究理事会;
关键词
D O I
10.1016/0960-894X(95)00111-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of several 2-pyridylthio-based pseudo-disaccharides (5 - 9) is described. One of them, them, 5a, shows inhibition of Agrobacterium beta-glucosidase (K-i = 800 mu M), possibly because in protonated form it mimics the protonated substrate (or transition state, compare I) lending to the glucopyranosyl cation.
引用
收藏
页码:763 / 766
页数:4
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