Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors

作     者：Wanjun Yan Wenming Li Decai Xiong Xinshan Ye 颜婉君;李文明;熊德彩;叶新山

作者机构：State Key Laboratory of Natural and Biomimetic DrugsSchool of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China 

基　　金：The National Key R&D Program of China(Grant No.2018YFA0507602) Project of National Science and Technology Major Project(Grant No.2019ZX09301-106) the National Natural Science Foundation of China(Grant No.91853122) 

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

年 卷 期：2020年第29卷第1期

页      码：29-44页

摘      要：A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linked *** inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’s HPLC-based *** synthetic compound 15 g showed moderate inhibitory *** findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.

主 题 词：Sialyltransferase inhibitor Carbamate Design Synthesis 

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

核心收录：

D　O　I：10.5246/jcps.2020.01.003

馆 藏 号：203878797...