酚羟基取代β-醛酮及其含糖类席夫碱衍生物的合成  

Synthesis and Antibacterial Activities of Aromatic β-aldehyde Ketone Schiff base Derivatives with Hydroxyl or Glycoside

作　　者：唐君源 刘进兵[1] 吴凤艳[1] 张超[1] 王子厚[1] 

机构地区：[1]邵阳学院生物与化学工程系,湖南邵阳422000

出　　处：《邵阳学院学报（自然科学版）》2016年第1期106-113,共8页Journal of Shaoyang University：Natural Science Edition

基　　金：研究生创新项目(CX2015SY009)

摘　　要：鱼腥草素具广谱的抗菌活性,其药效团为β-醛酮结构.以含有羟基的苯乙酮为起始原料,合成了8个羟基取代及含有糖苷的芳香β-醛酮席夫碱衍生物,所合成化合物经过红外、核磁进行了结构表征.对所合成的化合物进行了抑菌活性测试,初步构效关系表明,苯环上酚羟基取代对抗菌活性有重要影响,烷氧基胺席夫碱种类对抑菌活性影响很大,酮羰基的存在对提高抗菌活性有利.Houttuynine,n- nonyl- β- oxo- aldehyde,was isolated from Houttuynina cordata Thunb as the major active constituents,and the structure was characterized by having β- aldehyde ketone unit as important pharmacological moiety. Previous research showed that Houttuynin possesses broad spectrum pharmacological properties including antibacterial,antivirus,anti- inflammation and increasing immunity. 8 aromatic β- aldehyde ketone Schiff base derivatives with hydroxyl or glycoside were synthesized from 4'- Hydroxyacetophenone. All of the synthesized compounds were characterized by NMR and IR. Antibacterial activities of the synthesized compounds were measured. Preliminary structure- activity relationships showed that the kind of alkoxy amine Schiff base might be affect the antibacterial activities,the hydroxyl group is the active group,keto carbonyl might be beneficial to increase the antibacterial activities.

关 键 词：β-醛酮 糖苷 席夫碱 抗菌活性 

分 类 号：TQ645.6[化学工程—精细化工]