Abstract

Modified 1,5-dideoxy-1,5-imino-d-xylitol analogues with different substitution patterns involving position C-1 and/or the ring nitrogen were prepared, which were designed to serve as precursors for the preparation of iminoxylitol-based ligands and tools for the elucidation and modulation of human lysosomal β-glucocerebrosidase. Biological evaluation of the synthesized glycomimetics with a series of glycoside hydrolases revealed that these substitution patterns elicit excellent β-glucosidase selectivities.

Graphical abstract

中文翻译：

---

合成修饰的 1,5-亚氨基-d-木糖醇作为溶酶体 β-葡萄糖脑苷脂酶的配体。

摘要

制备了具有不同取代模式的修饰的 1,5-二脱氧-1,5-亚氨基-d-木糖醇类似物，涉及位置 C-1 和/或环氮，其被设计用作制备亚氨基木糖醇基配体的前体以及用于阐明和调节人类溶酶体β-葡萄糖脑苷脂酶的工具。用一系列糖苷水解酶对合成的糖模拟物进行生物学评估表明，这些取代模式引发了优异的β-葡萄糖苷酶选择性。

图形概要