| 张玲钰,李修刚,王玉丽,刘钰强,谢亚非,高志刚,魏鹏,徐为人,汤立达,赵桂龙.化学通报,2015,78(7):638-643. |
| 3,6-二脱氧达格列净的合成及其降血糖活性研究 |
| Synthesis and Hypoglycemic Activity of 3,6-Dideoxydapagliflozin |
| 投稿时间：2015-01-05 修订日期：2015-01-26 |
| DOI： |
| 中文关键词: 关 键 词 SGLT2抑制剂 二脱氧 合成 降血糖活性 |
| 英文关键词:SGLT2 inhibitor, Dideoxy, Synthesis, Hypoglycemic activity |
| 基金项目:国家自然科学基金(21302141)；天津市应用基础与前沿技术研究计划(14JCQNJC12900和14JCZDJC33500)；铜仁学院博士启动基金(trxyDF1401) |
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| 中文摘要: |
| 利用达格列净1作为原料经过两条路线合成了3,6-二脱氧达格列净9，其3,6-二脱氧的位置进一步经过了NOE技术确认，体外hSGLT2抑制试验和大鼠尿糖排泄试验表明3,6-二脱氧达格列净几乎没有SGLT2抑制活性，说明SGLT2抑制剂结构中葡萄糖片段上3-OH和6-OH同时脱除会导致SGLT2抑制剂完全丧失活性。 |
| 英文摘要: |
| 3,6-Dideoxydapagliflozin 9 was synthesized by two synthetic routes starting from dapagliflozin 1, whose 3,6-dideoxy functionality was further confirmed by NOE. In vitro inhibitory assay against hSGLT2 and rat urinary glucose excretion test found that 3,6-dideoxydapagliflozin 9 was almost completely inactive against hSGLT2, indicating that deletion of both 3-OH and 6-OH in the glucose moiety of SGLT2 inhibitors cannot be tolerated and would lead to complete loss of bioactivity. |
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