具有锁定功能的GLUT1高亲和力脑靶向文拉法辛前药的设计和合成
esign and Synthesis of 'Lock-in' Brain Targeted Prodrug of Venlafaxine With GLUT1 High Affinity
为了提高文拉法辛的脑靶向性，本文选择了血脑屏障上的葡萄糖转运蛋白1为载体，设计并合成了具有锁定功能的脑靶向性文拉法辛前药1。文中以文拉法辛为起始原料，通过桥链依次与TDS系统、硅基葡萄糖部分偶联，最后脱去保护基，得到目标化合物1，经1H NMR、IR 和MS 确证结构。
We reported a series of 'lock-in' brain-targeting Venlafaxine prodrugs utilizing the glucose transporter member 1 (GLUT1). Venlafaxine used as starting material was conjugated with TDS and 1,2,3,4-tetra-O-trimethysilyl-D-glucopyranose by different bicarboxyl acid, and then deprotected to afford the targeting compounds 1 which were conformed by 1H NMR, IR and MS.
吴勇、海俐、李晓岑
药学
药物化学葡萄糖转运体1脑靶向前药文拉法辛
Medicinal ChemistryGLUT1Brain TargetProdrugVenlafaxine
吴勇,海俐,李晓岑.具有锁定功能的GLUT1高亲和力脑靶向文拉法辛前药的设计和合成[EB/OL].(2014-09-24)[2025-08-02].http://www.paper.edu.cn/releasepaper/content/201409-314.点此复制
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