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  

Synthesis,Crystal Structure and Antimicrobial Activities of Novel Aroylhydrazones Containing Barbituric Acid Moiety

作　　者：冯洋[1] 李传碧[1] 赵丽婷[1] 李家琪[1] 魏亚男[1] 

机构地区：[1]吉林师范大学化学学院,吉林四平136000

出　　处：《应用化学》2016年第8期913-922,共10页Chinese Journal of Applied Chemistry

基　　金：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。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 heterocychc 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） of0. 8 g/L and against E. Coli with the MIC of 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 

分 类 号：O626.4[理学—有机化学]