含酰胺结构的苯基苯并噻唑基酮类衍生物的合成及生物活性  

Synthesis and bioactivity of benzothiazolylphenylmethanone derivatives containing amide

作　　者：饶家瑞 孟泽洪 李帅 张金峰 李悦欣 蒲运丹 周玉锋[1] RAO Jiarui;MENG Zehong;LI Shuai;ZHANG Jinfeng;LI Yuexin;PU Yundan;ZHOU Yufeng(Tea Research Institute,Guizhou Academy of Agricultural Sciences,Guiyang 550006,China)

机构地区：[1]贵州省农业科学院茶叶研究所,贵阳550006

出　　处：《农药》2023年第10期708-715,共8页Agrochemicals

基　　金：黔农科院青年基金[2022]29号。

摘　　要：[目的]设计、合成系列含酰胺结构的苯基苯并噻唑基酮类衍生物,以发掘活性优良的目标化合物用于防治小麦赤霉病、辣椒枯萎病和苹果腐烂病。[方法]将苯并噻唑引入二苯甲酮类杀菌剂的结构中合成不同取代基的衍生物,目标化合物的结构经过^(1)H NMR、^(13)C NMR、IR和元素分析进行表征。采用菌丝生长速率法测试目标化合物的离体抑菌活性,并通过盆栽试验测试化合物5f的活体保护和治疗活性。[结果]质量浓度为50 mg/L下化合物均表现出一定的抑菌活性,其中化合物5f对小麦赤霉病菌和辣椒枯萎病菌的抑制率为72.40%和70.20%,优于对照药剂霉灵;化合物5m对辣椒枯萎病菌和苹果腐烂病菌的抑制率为77.90%和74.20%,均比对照药剂霉灵高。在质量浓度300 mg/L下,化合物5f对对辣椒枯萎病的保护和治疗活性优于对照药剂霉灵。[结论]该类化合物具有一定的杀菌活性,可为二苯酮类杀菌剂的研究提供参考。[Aims]A series of benzothiazolylphenylmethanone derivatives containing amide structure were designed and synthesized to explore the target compounds with excellent activity for the control of Giberella zeae,Fusarium oxysporium and Cytospra mandshurica.[Methods]Benzothiazole was introduced into diphenylmethanone fungicide to synthesize derivatives having different substituents,and the structures of the target compounds were characterized by^(1)H NMR,^(13)C NMR,IR and elemental analysis.The in vitro fungicidal activity of the target compounds was tested by mycelial growth rate method,and the in vivo protection and curative activity of compound 5f was tested by pot experiment.[Results]The target compounds showed certain fungicidal activity at the concentration of 50 mg/L,with compound 5f having an inhibition rate of 72.40%and 70.20%against G.zeae and F.oxysporium,which was higher than that of control agent hymexazol.The inhibition rates of compound 5m against F.oxyspoirum and F.mandshurica were 77.90%and 74.20%,which were higher than that of hymexazol,too.At the concentration of 300 mg/L,the protective and curative activities of compound 5f against F.oxysporium were better than that of control agent hymexazol.[Conclusions]The target compounds having certain fungicidal activity provide a reference for the research of diphenylmethanone fungicides.

关 键 词：苯并噻唑 二苯甲酮 小麦赤霉病 辣椒枯萎病 苹果腐烂病 

分 类 号：TQ455.4[化学工程—农药化工]