| 邵艳东,王向辉,谢灵杰,门睿,林强.化学通报,2016,79(11):1058-1062. |
| 三芥子酸甘油酯类似物的合成及抑菌活性 |
| Synthesis and evaluation antibacterial activity of erucin analogs |
| 投稿时间：2016-03-18 修订日期：2016-04-18 |
| DOI： |
| 中文关键词: 三芥子酸甘油酯 合成 杀菌活性 |
| 英文关键词:erucin synthesis antibacterial activity |
| 基金项目:“十二五”国家科技支撑计划农药专项(2011BAE06B04-07)；海南省重点科技计划项目(ZDXM20120003)；海南省教育厅高等学校研究项目(HNKY2014-39) |
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| 中文摘要: |
| 以N-(2-溴乙基)邻苯二甲酰亚胺或N-(4-溴丁基)邻苯二甲酰亚胺和硫脲为起始原料,通过取代、肼解、亲核加成等反应经4步合成了10个三芥子酸甘油酯(erucin)类似物,通过核磁共振氢谱、碳谱及质谱对其结构进行了确认。采用比浊法初步测试了其对大肠杆菌、金黄色葡萄球菌、白色葡萄球菌、藤黄八叠球菌、枯草芽孢杆菌、蜡状芽孢杆菌和四联球菌等7种菌的生长抑制活性,测试结果显示化合物对测试菌种都表现出较好的生长抑制活性,其中苄硫乙基-1-硫代异硫氰酸酯(5e)和苄硫基丁基-1-硫代异硫氰酸酯(5j)活性最为突出,对大肠杆菌的最小生长抑制浓度仅为7.8 ug.mL-1,对金黄色葡萄球菌的生长抑制浓度也仅为15.6 ug/mL和 31.2 ug/mL。 |
| 英文摘要: |
| Ten erucin analogs were synthesized by four steps of substitution, aminolysis, and nucleophilic substitution reaction, starting from N-(2-bromoethyl)phthalimide or N-(4-bromobutyl)phthalimide. All the synthesized compounds were tested for their antimicrobial activity in vitro by turbidimetric method against Escherichia coli (DH5a), Staphylococcus aureus (ATCC25923), Staphylococcus albus (ATCC8799), Staphylococcus lutea (ACCC11001), Bacillus subtilis (ATCC6633), Bacillus cereus (ACCC11077) and Micrococcus tetragenus (ATCC35098). The results indicated that all the compounds exhibit good antimicrobial activity, benzyl(2-thiocyanatoethyl)sulfane (5e) and benzyl(4-thiocyanatobutyl)sulfane (5j) showed best inhibitory effects against Escherichia coli (DH5a), Minimum inhibitory concentration (MIC) is 7.8 μg/mL, and excellent inhibitory effects against Staphylococcus aureus (ATCC25923), MIC is 15.6μg/mL and 31.2μg/mL. |
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