| 新型含巴比妥酸的芳香酰腙类化合物的合成、晶体结构及抑菌活性 |
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| 引用本文： | 冯洋,李传碧,赵丽婷,李家琪,魏亚男. 新型含巴比妥酸的芳香酰腙类化合物的合成、晶体结构及抑菌活性[J]. 应用化学, 2016, 33(8): 913-922. DOI: 10.11944/j.issn.1000-0518.2016.08.150386 |
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| 作者姓名： | 冯洋 李传碧 赵丽婷 李家琪 魏亚男 |
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| 作者单位： | 吉林师范大学化学学院 吉林 四平 136000 |
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| 基金项目： | 吉林省科技厅基金资助项目(20140204080) |
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| 摘 要： | 在微波辅助下,1,3-二甲基-5-醛基巴比妥酸与芳氧基/芳胺基乙酰肼及含氮杂环乙酰肼缩合制备新型酰腙化合物,并对其抑菌活性进行评价的研究。 新化合物的结构经过元素分析、红外光谱、核磁共振谱、质谱和X射线单晶衍射等技术手段确认。 体外的抑菌活性实验显示,部分目标化合物呈现出优于环丙沙星的抑菌活性。 经过构效关系分析表明,当芳基为含氮杂环时,所形成的化合物抗菌活性与芳基为苯环时相比明显较强,抑菌活性最强的酰腙化合物2t对金黄色葡萄球菌的最小抑菌浓度(MIC)值为0.8 g/L,对大肠杆菌的最小抑菌浓度(MIC)值为1.6 g/L。
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| 关 键 词： | 巴比妥酸 芳香乙酰肼 微波辐射 晶体结构 抑菌活性 |
Synthesis,Crystal Structure and Antimicrobial Activities of Novel Aroylhydrazones Containing Barbituric Acid Moiety |
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| FENG Yang,LI Chuanbi,ZHAO Liting,LI Jiaqi,WEI Ya'nan. Synthesis,Crystal Structure and Antimicrobial Activities of Novel Aroylhydrazones Containing Barbituric Acid Moiety[J]. Chinese Journal of Applied Chemistry, 2016, 33(8): 913-922. DOI: 10.11944/j.issn.1000-0518.2016.08.150386 |
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| Authors: | FENG Yang LI Chuanbi ZHAO Liting LI Jiaqi WEI Ya'nan |
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| Affiliation: | Department of Chemistry,Jilin Normal University,Siping,Jilin 136000,China |
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| Abstract: | A series of novel acylhydrazone compounds was synthesized by a simple and efficient condensation of 1,3-dimethy-5-formyllbarbituric acids with aryloxy/arylamino acetylhydrazides and nitrogen-containing heterocyclic acetylhydrazides under microwave irradiation. The structures of all new compounds were confirmed by elemental analysis, IR, 1H NMR, mass spectrometry and single-crystal X-ray diffraction analysis. In vitro antimicrobial activity evaluation results show that some of the target compounds exhibit superior antimicrobial activities compared with ciprofloxacin. Structure-activity relationship analysis shows that when the aryl group is a nitrogen-containing heterocyclic compound, its antibacterial activity is significantly stronger than that of a benzene ring compound. One of target compounds 2t shows the strongest activities against S.Aureus with the minimum inhibitory concentration(MIC) of 0.8 g/L and against E.Coli with the MIC of 1.6 g/L. |
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| Keywords: | barbituric acid aryl acetohydrazide microwave irradiation crystal structure antimicrobial activity |
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