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1,4-二氧喹醛酸酯合成及抑菌活性研究
引用本文:马明真,李华.1,4-二氧喹醛酸酯合成及抑菌活性研究[J].中国兽药杂志,2016,50(6):26-32.
作者姓名:马明真  李华
作者单位:中国农业大学(烟台),中国农业大学(烟台)
基金项目:烟台市科技发展计划项目(2012ZH247)
摘    要:为了合成两种具有抑菌活性的1,4-二氧喹醛酸酯,即1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯和1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯,以苯并呋咱为原料,经Beirut反应、酯交换反应,合成了两种喹醛酸酯;1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯合成产率为29.3%,1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯合成产率为18.3%。两种1,4-二氧喹醛酸酯对大肠杆菌、金葡萄球菌、青霉菌和枯草杆菌均有明显的抑菌活性。通过测定产物的熔点和光谱分析证明系为所合成的目标产物。

关 键 词:苯并呋咱  酯交换反应  喹醛酸酯  抑菌活性
收稿时间:2016/3/19 0:00:00
修稿时间:2016/5/31 0:00:00

Study on the Synthesis and Bacteriostasis of 1,4-dioxide Quinoline aldehydes esters
Institution:China Agriculture University( Yantai),
Abstract:Using benzofuroxan as raw material , two kinds of 1,4-dioxide quinoline aldehydes esters , 1,4-dioxide quinoline-3- methyl -2- phenyl formate and 1,4-dioxide quinoline-3- methyl -2- cinnamyl formate , were synthesized by Beirut reaction and ester exchange reaction. The yield of 1,4-dioxide quinoline-3- methyl -2- phenyl formate was 29.3% and the yield of 1,4-dioxide quinoline-3- methyl -2- cinnamyl formate was 18.3%. Two kinds of 1,4-dioxide quinoline aldehyde ester have obvious antibacterial activity to Escherichia coli, Staphylococcus aureus, Penicillium sp. and Bacillus subtilis. It was proved that new compounds synthesized in experiment were target compounds by measuring the melting point and spectral analysis.
Keywords:benzofuroxan  ester exchange reaction  quinoline aldehydes esters  antibacterial activity
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