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
收稿日期: 2015-12-05
修回日期: 2016-01-28
网络出版日期: 2016-02-18
基金资助
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.
Ultrasonic Synthesis and Anti-phytopathogenic Fungi Activity Evaluation of 2-Sulfanylidene-2,3-dihydroquinazoline-4(1H)-one
Received date: 2015-12-05
Revised date: 2016-01-28
Online published: 2016-02-18
Supported by
Project supported by the Natural Science Basic Research Plan in Shaanxi Province (No. 2014JQ2064) and the Foundation for Young Scholars of Shaanxi University of Science & Technology (No. BJ12-26).
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、13C 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16 μg/mL, 优于阳性对照酮康唑.
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
张金 , 程佩 , 马养民 , 刘佳 , 苗智 , 范超 . 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[J]. 有机化学, 2016 , 36(6) : 1368 -1374 . DOI: 10.6023/cjoc201512008
In order to develop new potent anti-phytopathogenic fungi drugs, a series of 2-sulfanylidene-2,3-dihydroquinazo- line-4(1H)-ones were synthesized under ultrasonic irradiation. Structures of the compounds were characterized by IR, 1H NMR, 13C 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/mL, which showed significant inhibitory activity to Alternaria brassicae compared with that of the positive control drug ketoconazole.
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