| 曾 造,舒群威,李金海.化学通报,2018,81(1):83-87. |
| 去甲去氢斑蝥素酰亚胺缩水杨醛的合成及其性质研究 |
| Synthesis and Properties of Dehydronorcantharidin Imide-Salicylaldehyde |
| 投稿时间：2017-05-31 修订日期：2017-08-03 |
| DOI： |
| 中文关键词: 去甲去氢斑蝥素 水杨醛 合成 抑菌活性 荧光性质 |
| 英文关键词:Dehydronorcantharidin, Salicylaldehyde, Synthesis, Bacteriostatic activity, Fluorescence properties |
| 基金项目:中央高校基本科研业务费西南大学-毕节学院联合专项（XDJK2014C005），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（黔科合LH字[2015]7586号），贵州省山地友好型地膜开发重点实验室（黔教合KY字[2016]010号）和贵州省应用化学特色重点实验室（黔教合KY字[2011]004号）资助。 |
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| 中文摘要: |
| 以呋喃、水合肼和马来酸酐为原料，合成了去甲去氢斑蝥素酰亚胺缩水杨醛，其结构经NMR、MS和元素分析证实，并测定产物的抑菌活性及与牛血清蛋白(BSA)的相互作用。结果表明，标题化合物对大肠杆菌和金黄色葡萄球菌都有较好的抑菌活性，其对BSA为静态荧光猝灭，在293、303和310 K时猝灭常数分别是 3.39×104、3.29×104、3.13×104( L/mol)；化合物与BSA主要通过疏水作用力结合，其结合距离为2.688 nm，结合位点数为1.049(303 K)。 |
| 英文摘要: |
| In this work, dehydronorcantharidin imide-salicylaldehyde was synthesized from furan, maleic anhydride and hydrazine hydrate, and the structure of synthesized compound was confirmed by NMR, MS and elemental analysis. The bacteriostatic activity of the product and the interaction with bovine serum albumin (BSA) were tested. The results showed that the compound has good antibacterial activity against E.coli and S. aureus. The quenching mechanism of titled compound to BSA is static quenching. Moreover, at 293, 303 and 310 K, the quenching constants are 3.39×104 L/mol, 3.29×104 L/mol, 3.13×104 L/mol, respectively. The interaction of the compound to BSA is mainly driven by hydrophobic force. Meanwhile, the binding distance is 2.688 nm, and the number of binding sites is 1.049 (303 K). |
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