3-Oxodapagliflozin as a Potent and Highly Selective SGLT2 Inhibitor for the Treatment of Type 2 Diabetes
3-Oxodapagliflozin as a Potent and Highly Selective SGLT2 Inhibitor for the Treatment of Type 2 Diabetes作者机构：School of Chemistry and Chemical Engineering Shandong University Jinan 250100 P. R. China Tianjin Key Laboratory of Molecular Design and Drug Discovery Tianjin Institute of Pharmaceutical Research Tianjin 300193 P. R. China
出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)
年 卷 期：2014年第30卷第5期
页 面：785-793页
核心收录：
学科分类：0710[理学-生物学] 081902[工学-矿物加工工程] 0819[工学-矿业工程] 07[理学] 08[工学] 071007[理学-遗传学]
基 金：Supported by the National Natural Science Foundation of China(No.21302141) the Key Projects of Tianjin Science and Technolo- gy Support Plan China(No. 10ZCKFSH01300) and the Tianjin Municipal Natural Science Foundation China(No. 14JCQNJC 12900)
主 题：SGLT2 inhibitor Structure-activity relationship Dapagliflozin
摘 要：Structural modifications of 3-OH in the glucose moiety of dapagliflozin（1）, an approved potent sodium-dependent glucose transporter 2（SGLT2） inhibitor, led to 3-oxodapagliflozin（16）, a highly potent and more selective SGLT2 inhibitor[IC50（hSGLT1）/IC50（hSGLT2）=2851 for compound 16 vs. 843 for compound 1]. 3-Oxodapagliflozin（16） exhibited in vitro（IC50=1.0nmol/L against hSGLT2 for compound 16 vs. 1.3 nmol/L for compound 1） and in vivo activities comparable to those of dapagliflozin（1）. The bioactivities of 3-oxodapagliflozin （16） warrant its further evaluation as a promising SGLT2 inhibitor for the treatment of type 2 diabetes.
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