含1,2,4-三唑席夫碱的新型喹唑啉类化合物的合成及其抗菌活性研究
收稿日期: 2012-09-18
修回日期: 2012-11-09
网络出版日期: 2012-11-20
基金资助
贵州省农业科技攻关(No. 20093010)资助项目.
Synthesis and Fungicidal Activities of Novel Quinazoline Derivatives Containing 1,2,4-Triazole Schiff-Base Unit
Received date: 2012-09-18
Revised date: 2012-11-09
Online published: 2012-11-20
Supported by
Project supported by the Agricultural Science and Technology Foundation of Guizhou Province (No. 20093010).
以3-甲基-4-氨基-1,2,4-三唑-5-硫酮、芳醛和4-氯喹唑啉为原料, 经席夫碱和硫醚化反应合成了14个新型的含1,2,4-三唑席夫碱单元的喹唑啉类化合物6a～6n, 通过IR, 1H NMR, MS及元素分析对所合成的目标化合物进行了结构表征. 初步生物活性测试结果表明, 部分化合物表现出一定的抗菌活性. 在50 μg/mL浓度下, 化合物6g对辣椒枯萎菌、苹果腐烂菌及马铃薯晚疫菌的抑制率分别为71%, 72%和58%.
关键词： 1,2,4-三唑席夫碱; 喹唑啉; 合成; 抗菌活性
刘军虎 , 刘勇 , 蹇军友 , 鲍小平 . 含1,2,4-三唑席夫碱的新型喹唑啉类化合物的合成及其抗菌活性研究[J]. 有机化学, 2013 , 33(02) : 370 -374 . DOI: 10.6023/cjoc201209023
Using 3-methyl-4-amino-1,2,4-triazole-5-thione, aromatic aldehydes and 4-chloroquinazoline as starting materials, fourteen novel quinazoline derivatives containing 1,2,4-triazole Schiff-base unit were synthesized. The structures of target compounds were fully characterized by IR, 1H NMR, MS and elemental analysis. The preliminary bioassay showed that some compounds possessed certain fungicidal activities. At the concentration of 50 μg/mL, the inhibition rates of compound 6g against F. oxysporium, C. mandshurica and P. infestans were 71%, 72% and 58%, respectively.
Key words： 1,2,4-triazole Schiff-base; quinazoline; synthesis; fungicidal activity
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