苄氨基甲基黄酮化合物的合成和活性研究  

The Synthesis and Activity of Substituted Benzylamino Flavone Compounds

作　　者：凌新龙[1] 谢清若[1] 林海涛[1] 许金蓉[1] 

机构地区：[1]广西工学院,广西柳州545006

出　　处：《时珍国医国药》2012年第9期2229-2231,共3页Lishizhen Medicine and Materia Medica Research

基　　金：教育部科学技术研究重点项目(No.210163);广西壮族自治区自然科学基金(No.2010GXNSFA013045)

摘　　要：目的研究苄氨基甲基黄酮化合物的合成和活性。方法以苯酚和间甲基苯甲醛为原料,经酯化、重排、羟醛缩合、关环、卤代反应和氨化六步制备得到了5个N-苄氨基甲基黄酮,采用1H-NMR、FT-IR和MS对化合物进行结构鉴定;测试了它们对白色念珠菌(Candida albicans)、金黄色葡萄球菌(Staphylococcus aureus)和大肠埃希氏菌(Escherichia coli)3种细菌的抗菌活性。结果 5个N-苄氨基甲基黄酮化合物的产率分别为50.6%、30.1%、60.3%、51.2%和45.0%,其中4个苄氨基甲黄酮化合物对白色念珠菌有抑制作用,全部均对金黄色葡萄球菌有抑制作用,两个对大肠埃希氏菌有抑制作用。结论 5个N-苄氨基甲基黄酮化合物的合成路线方便,简单,产率高,可以用作抗菌药物。Objective To study the synthesis and activity of N - benzylaminomethyl flavones. Methods Phenol and 3 - methyl benzaldehyde as raw materials, five N - benzylaminomethyl flavones were synthesized by esterifieation, rearrangement, aldol con-densation, cyclization, halogenating reaction and ammonification. The structures of products were identified by ^1 H - NMR, FT - IR and MS spectra. Five of the new compounds were tested for their antimicrobial activity against Candida albicans, Staphylococcus au-reus and Escherichia coll. Results The yield of five N - benzylaminomethyl flavones reached 50.6% ,30.1% ,60.3% ,51.2% and 45.0% , respectively. Four N - benzylaminomethyl flavones had inhibition against Candida albieans. All had inhibition against Staphylococcus aureus. Two had inhibition against Escherichia coll. Conclusion The synthetic route of five N - benzylaminomethyl flavones has advantages of convenience, simple operation and high yield. They can be used for antibacterials.

关 键 词：苄氨基甲基黄酮 抗菌活性 合成 

分 类 号：O621.2[理学—有机化学]