Synthesis of allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-(1,2,3)-triazol-l-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido-β-D-glucopyranoside as a potential inhibitor of galectin-3

作     者：李晨 孟祥豹 金小锋 李中军 李庆 Chen Li;Xiang-Bao Meng;Xiao-Feng Jin;Zhong-Jun Li;Qing Li

作者机构：北京大学药学院天然药物及仿生药物国家重点实验室北京100191 

基　　金：National Natural Science Foundation of China(Grant No.20732001 and 90713004) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2008年第17卷第3期

页      码：209-214页

摘      要：Allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-（1,2,3）-triazol-1-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido- β-D-glucopyranoside, a potential inhibitor of galectin-3, was designed and synthesized using lactose as stating material. The modifications of lactose included in introducing of N-acetamino group at the C-2 position through an azidoiodoglycosylation meanwhile constructing the [3-aminolactoside stereoselectively and replacing 3＇-OH with substituent 1,2,3-triazolyl group to enhance the affinity toward galeetin-3.

主 题 词：Galectin-3 Inhibitor Azidoiodoglycosylation N-acetyllactosamine derivatives 

学科分类：1007[医学-药学类] 100701[100701] 10[医学] 

馆 藏 号：203727174...