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有机化学.pdfVIP

DOI: 10.6023/cjoc201209023 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 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 刘军虎 刘 勇 蹇军友 鲍小平* (贵州大学精细化工研究开发中心 教育部绿色农药与农业生物工程重点实验室 贵阳 550025) 摘要 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 Synthesis and Fungicidal Activities of Novel Quinazoline Derivatives Containing 1,2,4-Triazole Schiff-Base Unit Liu, Junhu Liu, Yong Jian, Junyou Bao, Xiaoping* (Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025) Abstract 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. Keywords 1,2,4-triazole Schiff-base; quinazoline; synthesis; fungicidal activity 喹唑啉类衍生物具有优良的生物活性,