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

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。

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

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.