Synthesis of modified 1,5-imino-d-xylitols as ligands for lysosomal β-glucocerebrosidase

Monatsh Chem. 2019;150(5):831-842. doi: 10.1007/s00706-019-02427-1. Epub 2019 May 11.

Abstract

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.

Keywords: Carbohydrates; Conformation; Enzymes; Iminoxylitol; β-Glucocerebrosidase; β-Glucosidase ligands.