| 肾靶向雷公藤内酯醇与2-氨基葡萄糖结合物的合成 |
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| 引用本文： | 刘畅,张志荣.肾靶向雷公藤内酯醇与2-氨基葡萄糖结合物的合成[J].华西药学杂志,2017,32(5). |
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| 作者姓名： | 刘畅 张志荣 |
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| 作者单位： | 四川大学华西药学院靶向药物与释药系统教育部重点实验室,四川成都,610041 |
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| 摘 要： | 目的 合成雷公藤内酯醇与2-氨基葡萄糖的结合物(TPG).方法 将雷公藤内酯醇与丁二酸酐反应生成雷公藤内酯醇丁二酸单酯,其游离羧基与2-脱氧-2-氨基-D-吡喃葡萄糖氨基乙苷1位上的氨基形成酰胺键,得到TPG前药,并鉴定其结构.结果 成功制备了TPG,其所含2-氨基葡萄糖具有肾靶向性,并改善了其水溶性.结论 该前药的合成路线可行性高,TPG具有肾靶向性,雷公藤内酯醇的水溶性得到了改善.
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| 关 键 词： | 雷公藤内酯醇 2-氨基葡萄糖 2-氨基葡萄糖衍生物 结合物 丁二酸酐 肾靶向 前体药物 水溶性 |
Synthesis of kidney-targeted prodrug triptolide-glucosamine conjugate |
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| LIU Chang,ZHANG Zhirong.Synthesis of kidney-targeted prodrug triptolide-glucosamine conjugate[J].West China Journal of Pharmaceutical Sciences,2017,32(5). |
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| Authors: | LIU Chang ZHANG Zhirong |
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| Abstract: | OBJECTIVE To synthesize triptolide-glucosamine conjugate (TPG) as a kidney-targeted prodrug.METHODS Triptolide was reacted with succinic anhydride to generate triptolide succinic acid monoester.Then the free carboxyl was connected to the 1-NH2 from the 2-glucosamine derivative 2-amino-1-(2-aminoethoxy)-glucose through amide bond.The compound was confirmed by NMR and HRMS.RESULTS Through this route,TPG was successfully synthesized.Because of the 2-glucosamine,TPG could target renal and its solubility was increased obviously.CONCLUSION The synthetic route is feasible.The prodrug TPG has renal targeting ability and better solubility. |
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| Keywords: | Triptolide 2-Glucosamine 2-Glucosamine derivative Conjugate Succinic anhydride Kidney-targeted Prodrug Solubility |
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