| 氮取代去甲斑蝥酰亚胺衍生物的合成及抗惊厥活性研究 |
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| 引用本文： | 李泳秀,孙晓飞,魏初铨. 氮取代去甲斑蝥酰亚胺衍生物的合成及抗惊厥活性研究[J]. 中南药学, 2008, 6(5): 549-552 |
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| 作者姓名： | 李泳秀 孙晓飞 魏初铨 |
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| 作者单位： | 苏州大学医学部药学院,江苏,苏州,215123 |
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| 摘 要： | 目的合成氮取代去甲斑蝥酰亚胺衍生物，发现新的抗惊厥先导化合物。方法呋喃和马来酐经过Diels—Alder反应生成去甲去氢斑蝥素，在钯炭催化下还原成去甲斑蝥素，与取代苯胺缩合成氮一苯基去甲斑蝥酰亚胺的衍生物。结果合成的大多数化合物都具有抗惊厥活性。结论化合物7、9和10可能成为新的抗惊厥先导化合物。
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| 关 键 词： | 去甲斑蝥素 去甲斑蝥酰亚胺 合成 抗惊厥 |
Synthesis and anticonvulsant activity of substituted N-phenyl derivatives of norcantharidimide |
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| LI Yong-xiu,SUN Xiao-fei,WEI Chu-quan. Synthesis and anticonvulsant activity of substituted N-phenyl derivatives of norcantharidimide[J]. Central South Pharmacy, 2008, 6(5): 549-552 |
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| Authors: | LI Yong-xiu SUN Xiao-fei WEI Chu-quan |
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| Affiliation: | (College of Pharmacy, Suzhou University, Suzhou Jiangsu 215123) |
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| Abstract: | Objective To synthesize N-phenyl substituents of norcantharidimide in order to find new anticonvulsant lead compounds. Methods Diels-Alder reaction between furan and maleic anhydride resulted in dehydronorcantharidin, and norcantharidin was obtained. Then norcantharidin was condensed with aniline derivatives to obtain the products. Results Most of the products had in subseqhent hydrogenation under Pd/C anticonvulsant activity. Conclusion Compounds 7, 9 and 10 may be the new anticonvulsant lead compounds. |
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| Keywords: | norcantharidin norcantharidimide synthesis anticonvulsant |
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