| 赵波,赵人杰,朱红.化学通报,2020,83(1):70-74. |
| 咪唑[1,5-a]吡啶鎓盐的合成、表征及生物活性测定 |
| Syntheses, Characterizations and Bioassay of Imidazo[1,5-a] Pyridinium Salts |
| 投稿时间：2019-08-15 修订日期：2019-09-19 |
| DOI： |
| 中文关键词: 离子液体 咪唑[1,5-a]吡啶鎓 抗菌性 |
| 英文关键词:Ionic liquid Imidazo[1,5-a] pyridinium salts Antibacterial activities |
| 基金项目:四川省科技创新苗子工程项目（2017063）资助 |
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| 中文摘要: |
| 通过三组份串联反应合成一系列咪唑[1，5-a]吡啶鎓盐，利用1H NMR、13C NMR、MS以及X射线单晶衍射确定其结构，其中以二乙烯三胺与三乙烯四胺为原料获得预期外的结构。以青霉素作为对照，研究了化合物的抗菌性。结果表明，所合成的化合物对溶壁微球菌和乙型链球菌均有抗菌效果，化合物2的抗菌效果最好；含有杂原子O的化合物3对嗜麦芽单胞菌和肺炎克雷伯氏菌的抗菌能力优于青霉素；联苯桥联的刚性双齿咪唑[1，5-a]吡啶鎓（5）比乙基桥联的柔性双齿咪唑[1，5-a]吡啶鎓（4）的抗菌性更强；化合物6为单齿大π体系芳香环，其抗菌效果较好，而化合物7和8为双齿的大π体系芳香环，其抗菌效果较弱。 |
| 英文摘要: |
| Imidazo[1,5-a] pyridinium salts were synthesized via a facile three-component coupling reaction. Their structures were confirmed by 1H NMR,13C NMR, MS and X-ray crystal diffraction analysis. Unexpected structures were obtained using diethylenetriamine and triethylenetetramine as raw materials. The antibacterial properties of the as-synthesized salts were studied by minimal inhibitory concentration (MIC) method using penicillin as a control. The results showed that all the compounds have antibacterial effect on Micrococcus lysococcus and Streptococcus B, and the antibacterial effect of compound 2 was the best. Compound 3 containing heteroatom O has stronger antibacterial activity against Maltophilia maltophilia and Klebsiella pneumoniae than that of penicillin. The biphenyl bridged bidentate imidazole[1,5-a]pyridinium salt (compound 5) has a better antibacterial effect than the ethyl bridged bidentate imidazole[1,5-a]pyridinium salt (compound 4). Compound 6 having a monodentate large π system aromatic ring has better antibacterial effect than that of compounds 7 and 8 containing a bidentate large π system aromatic ring. |
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