| 2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷的合成及其肝靶向应用研究 |
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| 引用本文： | 徐希明,余江南,傅志君,傅海珍,李青,尤启冬,张钧寿. 2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷的合成及其肝靶向应用研究[J]. 中国新药杂志, 2004, 13(3): 243-245 |
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| 作者姓名： | 徐希明 余江南 傅志君 傅海珍 李青 尤启冬 张钧寿 |
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| 作者单位： | 1. 江苏大学药学院,镇江,212001
2. 中国药科大学药学院,南京,210009 |
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| 基金项目： | 江苏省自然科学基金，江苏省青年科技人才基金 |
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| 摘 要： | 目的:合成具有肝靶向意义的2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷,并考察其肝脏靶向性能.方法:以半乳糖为起始物,经乙酰化、溴代、缩合、置换,加醇后得目的化合物.小鼠尾静脉注射给药后,HPLC测定药物在小鼠肝脏及血液中的浓度.结果:目标化合物经IR和MS进行了结构确证.白蛋白微球表面偶联2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷,肝靶向效率增大约1.5倍.结论:所制半乳糖白蛋白微球趋肝性能增强.
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| 关 键 词： | 2-亚氨基-2-甲氧基乙基-1-硫代-β-D-半乳吡喃糖苷 肝靶向 微球 |
| 文章编号： | 1003-3734(2004)03-0243-03 |
Synthesis of 2-imino-2-methoxyethyl-1-thio-galactose and application for liver targeting |
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| XU Xi-ming,YU Jiang-nan,FU Zhi-jun,FU Hai-zhen,LI Qing,YOU Qi-dong,ZHANG Jun-shou. Synthesis of 2-imino-2-methoxyethyl-1-thio-galactose and application for liver targeting[J]. Chinese Journal of New Drugs, 2004, 13(3): 243-245 |
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| Authors: | XU Xi-ming YU Jiang-nan FU Zhi-jun FU Hai-zhen LI Qing YOU Qi-dong ZHANG Jun-shou |
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| Abstract: | Objective:To synthesize 2-imino-2-methoxyethyl -1-thio-galactose and to observe its effect on liver targeting. Methods: 2-imino-2-methoxyethly-l-thio-galactose was synthesized from galactose by a series reaction including acetylation, bromization, condensation, substitution and addition with methanol. After intravenous injection to mice,the concentration of drug in mice plasma and liver was determined by HPLC. Results:The product was identified by IR,MS techniques. Targeting efficiency for liver increased about 1. 5 fold, after 2-imino-2-methoxyethyl-l- thio-galactose reacted successfully on the surface of albumin microspheres. Conclusion: Galactosyl albumin microspheres showed remarkable targeting for liver. |
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| Keywords: | 2-imino-2-methoxyethyl-l-thio-galactose liver targeting microspheres |
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