含三氮唑、噻二唑的酰胺化合物的设计、合成及除草活性  

Design,synthesis and herbicidal activity of amide derivatives containing triazole and thiadiazole

作　　者：郭洋洋[1] 刘英 郑广进[1] 张海全[1] 蔡杰慧 唐小强 陆世大 覃旭兵 王强[1] GUO Yang-yang;LIU Ying;ZHENG Guang-jin;ZHANG Hai-quan;CAI Jie-hui;TANG Xiao-qiang;LU Shi-da;QIN Xu-bing;WANG Qiang(Chemical and Biological Engineering,Guangxi Normal University for Nationalities,Chongzuo 532200,Guangxi,China)

机构地区：[1]广西民族师范学院化学与生物工程学院,广西崇左532200

出　　处：《农药》2022年第12期873-876,共4页Agrochemicals

基　　金：广西民族师范学院2021年校级科研项目(2021YB038);广西民族师范学院大学生创新创业训练项目(S202110604169)。

摘　　要：[目的]设计并合成一系列含三氮唑、噻二唑结构的酰胺类化合物,以发现新的优良除草类化合物。[方法]运用活性结构拼接原理设计合成含杂环类化合物,以5-甲基噻吩-2-甲酸、硫代氨基脲、有机酸为起始原料,经过7步反应合成目标化合物。化合物的结构用^(1)H NMR、^(13)C NMR和HRMS表征确认,采用油菜平皿法测试化合物的除草活性。[结果]总共合成10个杂环化合物,初步除草活性试验结果表明:目标化合物对牛筋草、青葙子、刺苋具有较好的活性,特别是化合物3c、3e对牛筋草的抑制效果优于同等剂量下的阳性药。[结论]部分化合物除草活性优异,可作为除草先导化合物进一步研究。[Aims]This study aims to discover potent compounds with high herbicidal activities by designing and synthesizing a series of novel amide derivatives containing triazole and thiadiazol moiety.[Methods]According to the active structure combination principle,the target compounds were synthesized successfully from starting materials5-methylthiophene-2-formic acid,thiocarbazide and acid via 7 steps of reactions.The structures of products were characterized and confirmed by ^(1)H NMR,^(13)C NMR and HRMS,while the herbicidal activities were determined by using plate method.[Results]10 Heterocyclic compounds were synthesized in total.Preliminary results of herbicidal activity indicated that target compounds showed potential inhibitory activity against Eleusine indica(L.)Gaertn.,Lysimachia barystachys Bunge and Amaranthus spinosus L.In particular,compounds 3c,3e showed better activity against E.indica(L.)Gaertn.than the control agent at the same dose.[Conclusions]Some target compounds showed potential herbicidal activities and could be further investigated.

关 键 词：合成 噻吩 三氮唑 噻二唑 除草活性 

分 类 号：TQ460.3[化学工程—制药化工]