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去甲去氢斑蝥素酰亚胺衍生物的合成及抑菌活性
引用本文:曾造,李金海,舒群威,吕敬松. 去甲去氢斑蝥素酰亚胺衍生物的合成及抑菌活性[J]. 化学试剂, 2017, 39(11). DOI: 10.13822/j.cnki.hxsj.2017.11.005
作者姓名:曾造  李金海  舒群威  吕敬松
作者单位:贵州工程应用技术学院化学工程学院贵州省应用化学特色重点实验室,贵州毕节,551700
基金项目:西南大学-毕节学院联合基金项目,贵州省科学技术厅、毕节市科学技术局、贵州工程应用技术学院科学技术联合基金项目,贵州省山地友好型地膜开发重点实验室资助项目,贵州省应用化学特色重点实验室资助项目
摘    要:以顺丁烯二酸酐和呋喃为起始原料,经Diels-Alder、取代和缩合反应,合成了7个去甲去氢斑蝥素酰亚胺衍生物,其结构经NMR和元素分析证实。通过滤纸片法分别测定合成物对大肠杆菌、金黄色葡萄球菌的抑菌活性。结果表明,中间体N-氨基去甲去氢斑蝥素酰亚胺和部分产物对两种细菌都有较好的抑菌活性。其中,N-(氨基缩对甲氧基苯甲醛)-去甲去氢斑蝥素酰亚胺对大肠杆菌的抑菌活性最强,抑菌圈直径为28 mm。

关 键 词:去甲去氢斑蝥素  酰亚胺衍生物  合成  抑菌活性

Synthesis and Bacteriostatic Activity of Dehydronorcantharidin Imide Derivatives
ZENG Zao,LI Jin-hai,SHU Qun-wei,LV Jing-song. Synthesis and Bacteriostatic Activity of Dehydronorcantharidin Imide Derivatives[J]. Chemical Reagents, 2017, 39(11). DOI: 10.13822/j.cnki.hxsj.2017.11.005
Authors:ZENG Zao  LI Jin-hai  SHU Qun-wei  LV Jing-song
Abstract:In this work,seven dehydronorcantharidin imide derivatives were synthesized through Diels-Alder,substitution and condensation from furan and maleic anhydride.The structures of synthetic compounds were confirmed by NMR and elemental analysis.The bacteriostatic activity of synthetic compounds against Escherichia coli and Staphylococcus aureus were tested by the method of filter-paper.The result shown that the N-amino dehydronorcantharidin and some compounds against two bacteria had obvious antibacterial activity.Especially,N-amino-4-methoxybenzaldehyde dehydronorcantharidin against Escherichia coli was the best,and the inhibition zone diameter was 28 mm.
Keywords:dehydronorcantharidin  imide derivatives  synthesis  bacteriostatic activity
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