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.
出处
《时珍国医国药》
CAS
CSCD
北大核心
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)
关键词
苄氨基甲基黄酮
抗菌活性
合成
Benzylaminomethyl Flavonc
Antibacterial Activity
Synthesis
