中文关键词:吡啶咪唑啉酮合成抑菌活性 英文关键词:pyridine, imidazolone, synthesis, antifungalactivity 基金项目:山东省自然科学基金 (No. ZR2014BM030)

作者	单位	E-mail
张君辉	山东农业大学化学与材料科学学院 泰安 271018	1170570053@qq.com
刘思	山东农业大学化学与材料科学学院 泰安 271018
时艳华	山东农业大学化学与材料科学学院 泰安 271018
姜林	山东农业大学化学与材料科学学院 泰安 271018	jiangl@sdau.edu.cn

摘要点击次数:1613 全文下载次数:0 中文摘要: 本文以2-硫代乙内酰脲、取代苯甲醛、碘甲烷、吡啶甲胺等为原料,经Knoevenagel缩合、甲基化、取代三步反应,合成了一系列5-取代苯亚甲基-2-[(吡啶-3-基)甲氨基]-1H-咪唑-4(5H)-酮(3a ~ 3i),其结构经IR、₁H NMR、₁₃C NMR和HRMS确证。抑菌活性试验表明,在药剂浓度为100μg/mL时,目标化合物对灰霉菌均有中等抑制活性,抑制率69.5% ~ 83.2%之间；在相同浓度下大部分对菌核菌有较高的抑制活性,抑制率为87.9% ~ 100%, 其活性高于对照药剂三唑酮和百菌清。 英文摘要: A series of 5-substituted benzylidene-2-[(pyridine-3-yl)methylamino]-1H-imidazol-4(5H)-ones (3a ~ 3i) were synthesized by Knoevenagel condensation, methylation and substitution reactions using 2-thiohydantoin, substituted benzaldehydes, methyl iodide and pyridin-3-ylmethyl amine as starting materials. The structures of the target compounds were characterized by IR, ₁H NMR, ₁₃C NMR and HRMS. Meanwhile, their in vitro antifungal activities were evaluated, and the results indicated that the target compounds had moderate activities against B. cinerea with inhibition rates of 69.5% ~ 83.2% at 100μg/mL; most compounds exhibited notable activities against S. sclerotiorum with inhibition rates of 87.9% ~ 100% at the same dosage, which were higher than that of the control fungicides, triazolone and chlorothalonil. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书 -->