| 张君辉,刘思,时艳华,姜林.化学通报,2018,81(3):248-253. |
| 2-[(吡啶-3-基)甲氨基]-1H-咪唑-4(5H)-酮衍生物的合成及其抑菌活性 |
| Synthesis and Antifungal Activity of2-[(Pyridin-3-yl)methylamino]-1H-imidazol-4(5H)-one Derivatives |
| 投稿时间：2017-10-25 修订日期：2017-12-10 |
| DOI： |
| 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, antifungal activity |
| 基金项目:山东省自然科学基金 (No. ZR2014BM030) |
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| 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. |
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