以D-葡萄糖为载体的布洛芬脑靶向前体药物的设计与合成
Design and synthesis of Ibuprofen prodrugs for brain target delivery using D-glucose as a vector
作者:刘兴;李文浩;龚涛;
Author:
收稿日期: 年卷(期)页码:2013,28(01):-26-28
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:脑靶向;D-葡萄糖;非甾体抗炎药;合成
Key words:
基金项目:
中文摘要
目的设计并合成以葡萄糖转运体为靶细胞的脑靶向前体药物。方法将非甾体抗炎药布洛芬通过不同的桥链(1,6-己二醇和1,12-十二二醇)与D-葡萄糖通过共价键连接起来。结果成功合成了两个以D-葡萄糖为载体的脑靶向前体药物。结论目标化合物已经1HNMR、MS确证。
参考文献
[1]Pardridge W.Brain metabolism:A perspective from the blood-brain barrier[J].Physiol Rev,1983,63:1481-1535.
[2]Battaglia G,La Russa M,Bruno V,et al.Systemically adminis-tered d-glucose conjugates of 7-chlorokynurenic acid are cen-trally available and exert anticonvulsant activity in rodents[J].Brain Res,2000,860:149-156.
[3]Bonina F,Puglia C,Rimoli MG,et al.Synthesis and in vitrochemical and enzymatic stability of glycosyl 3'-azido-3'-deoxythymidine derivatives as potential anti-HIV agents[J].Eur J Pharm Sci,2002,16:167-174.
[4]Halmos T,Santarromana M,Antonakis K,et al.Synthesis of glu-cose-chlorambucil derivatives and their recognition by the hu-man GLUT1 glucose transporter[J].Eur J Pharmacol,1996,318:477-484.
[5]Halmos T,Santarromana M,Antonakis K,et al.Synthesis of O-methylsulfonyl derivatives of d-glucose as potential alkylatingagents for targeted drug delivery to the brain.Evaluation of theirinteraction with the human erythrocyte GLUT1 hexose transporter[J].Carbohyd Res,1997,299:15-21.
[6]Amigues EJ,Greenberg ML,Ju S,et al.Synthesis ofcyclophospho-glucoses and glucitols[J].Tetrahedron,2007,63:10042-10053.
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