A Selectiveα-L-Fucosidase Inhibitor Based on an Aminocyclopentane Framework
A Selectiveα-L-Fucosidase Inhibitor Based on an Aminocyclopentane Framework
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基于氨基环戊烷框架的选择性α-L-岩藻糖苷酶抑制剂
DOI：
10.1002/(sici)1522-2675(19990505)82:5
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发表时间：
1999
影响因子：
1.8
通讯作者：
J. Reymond
中科院分区：
文献类型：
--
作者：
A. Blaser;J. Reymond
(1R以D-核糖为原料，立体选择性地制备了（2 R，3R，4S，5 R）-4-氨基-5-甲基环戊烷-1，2，3-三醇（1）。氨基环戊烷三醇1，根据其设计可被视为岩藻糖基阳离子的类似物，相对于α-和β-葡萄糖苷酶、α-和β-甘露糖苷酶以及α-和β-半乳糖苷酶，选择性抑制α-L-岩藻糖苷酶（Ki=28 μM）（表）。
(1R,2R,3R,4S,5R)-4-amino-5-methylcyclopentane-1,2,3-triol (1) was prepared stereoselectively from D-ribose (Scheme). Aminocyclopentanetriol 1, which by its design may be considered an analog of the fucosyl cation, inhibits α-L-fucosidase selectively (Ki=28 μM) over α- and β-glucosidase, α- and β-mannosidase, and α- and β-galactosidase (Table).