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新型胆酸不对称双缩二氨基硫脲类衍生物的合成及其抗菌活性 被引量：2

Synthesis and Antibacterial Activities of Novel Cholic Acid Asymmetric Bis Thiosemicarbazone Derivatives
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摘要 在微波辐射条件下,甾酮与取代单缩二氨基硫脲经缩合反应合成了12个新型的胆酸不对称双缩二氨基硫脲衍生物(3a^3l),其结构经1H NMR,IR,ESI-MS和元素分析表征。初步抗菌活性测定结果表明:部分化合物对枯草芽孢杆菌、金黄色葡萄球菌、大肠杆菌及绿脓杆菌有一定的抗菌活性,其中,1-(2-羟基苯苄叉基)-5-[3-(3,7-二氧代-24-胆烷酸甲酯)亚甲基]二氨基硫脲(3f)对大肠杆菌的抑菌活性(IC507.40)与阿莫西林(IC507.30)相当。 Twelve novel cholic acid asymmetric bis thiosemicarbazone derivatives（3a-31） were syn- thesized by condensation of steroidal ketones with substituted thiosemicarbazides under microwave ir- radiation. The structures were characterized by 1H NMR, IR, ESI-MS and elemental analysis. Pre- liminary antibacterial activities tests indicated）that some compounds exhibited certain inhibitory activi- ties against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomanus aeroginosa. 1- （2-Hydroxybenzylidene） -5- [ 3- （7,12-dioxo-24-cholanate） methylene ] thiocarbohydrazide （3f） showed inhibitory activities（ IC50 7.40） as same as Amoxicillin（ IC50 7.30） against Escherichia coli.
作者 张丽娜 赵志刚 谭炯 李晖
机构地区 西南民族大学化学与环境保护工程学院
出处 《合成化学》 CAS CSCD 2015年第8期677-682,共6页 Chinese Journal of Synthetic Chemistry
基金 四川省科技支撑计划项目(2012SZ0160) 西南民族大学研究生创新型科研项目(CX2014SZ43)
关键词 胆酸 缩氨基硫脲 微波合成 抗菌活性 cholic acid thiosemicarbazone microwave synthesis antibacterial activity
分类号 O621.3 [理学—有机化学] O629.2 [理学—有机化学]
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参考文献28

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二级参考文献175

共引文献59

同被引文献21

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合成化学
2015年 第8期

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