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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
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
作者姓名:冯洋  李传碧  赵丽婷  李家琪  魏亚男
作者单位:吉林师范大学化学学院 吉林 四平 136000
基金项目:吉林省科技厅基金资助项目(20140204080)
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。

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
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
Authors:FENG Yang  LI Chuanbi  ZHAO Liting  LI Jiaqi  WEI Ya'nan
Affiliation:Department of Chemistry,Jilin Normal University,Siping,Jilin 136000,China
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.
Keywords:barbituric acid  aryl acetohydrazide  microwave irradiation  crystal structure  antimicrobial activity
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