吩嗪-1-羧酸双酰肼衍生物的合成、杀菌活性及韧皮部的输导.PDFVIP

农药学学报 2017, 19(3): 290-297 Chinese Journal of Pesticide Science • 研究论文 • DOI: 10.16801/j.issn.1008-7303.2017.0038 吩嗪-1-羧酸双酰肼衍生物的合成、杀菌活性及 韧皮部的输导性研究 柳 豪, 余林花, 熊志鹏, 张 敏, 李俊凯, 徐志红, 吴清来* (长江大学 农学院/农药研究所，湖北 荆州 434025) 摘 要：天然产物吩嗪-1-羧酸 (PCA ，申嗪霉素) 及其衍生物吩嗪-1- 甲酰肼具有独特的化学结构 和优良的杀菌等生物活性，但均没有韧皮部输导性。本文以具有抑菌活性的吩嗪-1-羧酸和具有 韧皮部输导性的马来酰肼为先导化合物，将马来酰肼中的双酰肼结构引入到吩嗪-1-羧酸中，设 计、合成了 17 个新化合物，其结构均经过核磁共振氢谱、高分辨质谱及 X-射线单晶衍射分析 确证。初步生物活性测试表明：大部分目标化合物在 50 mg/L 下对水稻纹枯病菌 Thanatephorus cucumeris 表现出中等偏上的抑制活性，其中化合物 6m 的抑制率达 92% 。但输导性研究结果显 示，目标化合物没有明显的韧皮部输导性。 关键词: 吩嗪-1-羧酸 ( 申嗪霉素)；马来酰肼；双酰肼；合成；杀菌活性；韧皮部输导性 中图分类号：O626.417 ；S482.2 文献标志码：A 文章编号：1008-7303(2017)03-0290-08 Synthesis, fungicidal activity and phloem mobility of phenazine- 1-carboxylic acid diacylhydrazine derivatives LIU Hao, YU Linhua, XIONG Zhipeng, ZHANG Min, LI Junkai, XU Zhihong, WU Qinglai* (College of Agriculture, Institute of Pesticides , Yangtze University, Jingzhou 434025, Hubei Province, China) Abstract: Phenazine-1-carboxylic acid (PCA, Shenqinbactin) and its derivative phenazine-1-carboxylic hydrazine are natural products that have been characterized to have unique chemical structures and interesting bioactivities. However, neither of them has phloem mobility. In this paper, phenazine-1- carboxylic acid and maleic hydazide were used as the corporate lead compounds which were introduced into the diacylhydrazine scaffold, and17 new compounds were de