超声辐射法合成2-硫亚基喹唑啉-4(1H)-酮类化合物及其抗植物病原菌活性研究  

Ultrasonic Synthesis and Anti-phytopathogenic Fungi Activity Evaluation of 2-Sulfanylidene-2,3-dihydroquinazoline-4(1H)-one

作　　者：张金[1] 程佩[1] 马养民[1] 刘佳[1] 苗智[1] 范超[1] 

机构地区：[1]陕西科技大学化学与化工学院教育部轻化工助剂化学与技术重点实验室,西安710021

出　　处：《有机化学》2016年第6期1368-1374,共7页Chinese Journal of Organic Chemistry

基　　金：陕西省科技厅自然科学基础研究计划(No.2014JQ2064);陕西科技大学博士科研启动基金(No.BJ12-26)资助项目~~

摘　　要：为了寻找更好的抗植物病原菌药物,采用超声辐射法合成了一系列的2-硫亚基喹唑啉-4(1H)-酮类化合物,所得化合物均被~1H NMR、^(13)C NMR、IR以及MS表征确认.并将所得化合物3a^3m采用最小抑菌浓度法对9种植物病原菌进行了抗真菌活性测试,发现大部分化合物对白菜黑斑病菌(Alternaria brassicae)和葡萄炭疽病菌(Colletotrichum gloeosporioides)有很强的抑制作用.其中化合物3a、3b、3g、3h对白菜黑斑病菌(Alternaria brassicae)的最小抑菌浓度达到16μg/m L,优于阳性对照酮康唑.In order to develop new potent anti-phytopathogenic fungi drugs, a series of 2-sulfanylidene-2,3-dihydroquinazoline-4（1H）-ones were synthesized under ultrasonic irradiation. Structures of the compounds were characterized by IR, ~1H NMR, ^（13） C NMR and MS. All compounds were investigated for anti-phytopathogenic fungi activity via the method of minimum inhibitory concentrations. The majority of compounds exhibited a good inhibitory activity to Alternaria brassicae and Colletotrichum gloeosporioides. The minimum inhibitory concentrations of compounds 3a, 3b, 3g and 3h were 16 μg/m L,which showed significant inhibitory activity to Alternaria brassicae compared with that of the positive control drug ketoconazole.

关 键 词：超声辐射 2-硫亚基喹唑啉-4(1H)-酮 抗植物病原菌活性 最小抑菌浓度 

分 类 号：O626[理学—有机化学] TQ450.1[理学—化学]