Synthesis of novel N-glycoside derivatives via CuSCN-catalyzed reactions and their SGLT2 inhibition activities
Synthesis of novel N-glycoside derivatives via CuSCN-catalyzed reactions and their SGLT2 inhibition activities
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DOI：
10.1016/j.tet.2015.05.108
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发表时间：
2015-07-29
期刊：
影响因子：
2.1
通讯作者：
Ye, Xin-Shan
中科院分区：
文献类型：
--
作者：
Bai, Shao-Tao;Xiong, De-Cai;Ye, Xin-Shan
首次通过cuscn催化的点击反应和ullmann型偶联反应合成了新型三唑- n-糖苷衍生物。对这些合成的n -苷类化合物的SGLT2抑制活性进行了评价，部分化合物在100 nM处表现出中等的SGLT2抑制活性。这一结果可能有助于发现新的用于治疗糖尿病的SGLT2抑制剂。(C) 2015 Elsevier Ltd.版权所有。
A convenient approach to the synthesis of novel triazole-N-glycoside derivatives was developed via CuSCN-catalyzed click reaction and Ullmann-type coupling reaction for the first time. The SGLT2 inhibitory activities of these synthetic N-glycosides were evaluated, and some compounds showed moderate SGLT2 inhibition activities at 100 nM. The results could benefit the discovery of new SGLT2 inhibitors for the treatment of diabetes. (C) 2015 Elsevier Ltd. All rights reserved.