文章摘要
孙跃,霍新玉,王兆旭,韩小强,张洁.苯并咪唑桥连的双-β-咔啉衍生物的合成与生物活性[J].精细化工,2020,37(8):
苯并咪唑桥连的双-β-咔啉衍生物的合成与生物活性
Synthesis and biological activity of bis-β-carboline derivatives containing benzimidazole structural unit
投稿时间:2020-04-01  修订日期:2020-05-10
DOI:
中文关键词: 苯并咪唑  双-β-咔啉  合成  抑菌活性  构效关系
英文关键词: benzimidazole  bis-β-carboline  synthesis  fungicidal activity  structure-activity relationship
基金项目:国家大学生创新创业训练计划项目(201810759055),新疆维吾尔自治区研究生科研创新项目(XJGRI2017045)
作者单位E-mail
孙跃 石河子大学化学化工学院 sy15522709052@163.com 
霍新玉 石河子大学化学化工学院  
王兆旭 石河子大学化学化工学院  
韩小强 石河子大学农学院  
张洁 School of Chemistry and Chemical Engineering/Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan, Shihezi University zhangjie-xj@163.com 
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中文摘要:
      为寻找高活性的新农药先导化合物,以1-取代的-β-咔啉-3-羧酸乙酯为原料,经过烷基化、还原、氧化等4步反应,合成10个以苯并咪唑桥连的双-β-咔啉衍生物,所合成的目标化合物经核磁共振氢谱、核磁共振碳谱和高分辨质谱确证其结构。并采用菌丝生长速率法测试了目标化合物对棉花枯萎病原菌、棉花立枯丝核菌、向日葵菌核、油菜菌核和葡萄灰霉病原菌的抑菌活性。离体杀菌活性测定结果表明,在50 mg/L下,目标化合物对测试的5种病原菌显示出一定抑制活性,其中化合物Ⅴb和Ⅴi对向日葵菌核的抑制率分别为100%和92.4%。该类化合物可以为设计研究新型农用杀菌剂提供参考。
英文摘要:
      In order to find novel pesticide leading compound with high bioactivity, ten bis-β-carboline derivatives linked by benzimidazole were synthesized starting from ethyl 1-substituted-β-carboline-3- carboxylate via alkylation, oxidation, and condensation. The structure of all novel compounds was confirmed by 1H NMR, 13C NMR and HRMS. Their antifungal activities were evaluated in vitro against five phytopathogenic fungi (Cotton Fusarium, Rhizoctonia solani, Sunflower sclerotinia, Rape sclerotinia, and Botrytis cinerea) using myvelium growth rate method. The preliminary results showed that most of the compounds possessed some fungicidal activity to five phytopathogenic fungi at 50 mg/L. These compounds have exhibited a significant inhibitory effect against sunflower sclerotinia rot in which compounds Ⅴb, and Ⅴi had inhibitory rates of 100%, and 92.4%, respectively. The information obtained from the studies may be useful for the design of novel agricultural fungicides.
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