Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors
Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors
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含氨基甲酸酯唾液酸转移酶抑制剂的设计、合成及评价
DOI：
10.5246/jcps.2020.01.003
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发表时间：
2020-01
影响因子：
--
通讯作者：
Ye Xinshan
中科院分区：
文献类型：
--
作者：
Yan Wanjun;Li Wenming;Xiong Decai;Ye Xinshan
设计并合成了一系列含氨基甲酸酯的唾液酸转移酶抑制剂来模拟磷酸盐连接的 CMP-Neu5Ac。使用基于 Schmidt HPLC 的测定法测定了它们对重组人 ST3Gal I 和 ST6Gal I 的抑制活性。合成化合物15g显示出中等的抑制活性。这些发现表明，氨基甲酸酯可以作为唾液酸转移酶抑制剂设计中磷酸基团的生物电子等排替代物，以改善膜的通透性。
A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linked CMP-Neu5Ac. Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt's HPLC-based assay. The synthetic compound 15g showed moderate inhibitory activity. These findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.