N-(苯基)噻唑酰胺类衍生物的合成及杀菌活性  

Synthesis and Fungicidal Activity of The N-(Phenyl)Thiazolamide Derivatives

作　　者：张勇 时锦超[1,2] 胡勇 廖灿 王美美 朱祥 余林花[1,2] 李俊凯 Yong;SHI Jinchao;HU Yong;LIAO Can;WANG Meimei;ZHU Xiang;YU Linhua;LI Junkai(School of Agriculture,Yangtze University,Jingzhou 434025,China;Institute of Pesticides,Yangtze University,Jingzhou 434025,China;Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Guizhou University,Guiyang 550025,China)

机构地区：[1]长江大学农学院,湖北荆州434025 [2]长江大学农药研究所,湖北荆州434025 [3]贵州大学绿色农药与农业生物工程国家重点实验室培育基地/教育部重点实验室,贵州贵阳550025

出　　处：《合成化学》2024年第2期150-157,共8页Chinese Journal of Synthetic Chemistry

基　　金：大学生创新创业训练计划项目(YZ2022198);中国博士后科学基金资助项目(2022M710917);国家自然科学基金资助项目(2018YFD0200500)。

摘　　要：为了寻求以天然产物为先导结构的绿色、高效新型杀菌剂,以苯甲腈、3-溴丙酮酸乙酯和不同取代苯胺为原料,通过活性亚结构拼接合成了12个N-(苯基)噻唑酰胺类衍生物(6a~6l)。产物结构均经过^(1)H NMR、^(13)C NMR和HR-MS(MSI)表征。杀菌活性结果显示:该类化合物对水稻纹枯病菌、白芨白绢病菌和水稻稻瘟病菌有良好的抑制作用。化合物6c和6l对水稻稻瘟病菌的EC_(50)值分别为0.015 mmol/L和0.020 mmol/L,优于对照药剂申嗪霉素(EC_(50)=0.031 mmol/L),其作为以天然产物为先导结构的新型杀菌剂,值得进一步探索研究。Seeking green,high-efficiency new fungicides with natural products as the leading structure.Using benzonitrile,ethyl 3-bromopyruvate,and different substituted anilines as raw materials,a series of twelve N-(phenyl)thiazole amide derivatives(6a~6l)were synthesized by splicing active substructures.And confirmed by^(1)H NMR,^(13)C NMR,and HR-MS(MSI)analysis.The results of fungicidal activity showed that the compounds had remarkable antifungal activity on R.solani,S.rolfii.and M.oryzae,and the EC_(50)values of compounds 6c and 6l against M oryzae were 0.015 mmol/L and 0.020 mmol/L better than the commercial fungicide phenazine-1-carboxylic acid(EC_(50)=0.031 mmol/L).Compounds 6c and 6l can be used as a new fungicide with natural products as the lead structure and deserves further exploration.

关 键 词：噻唑 酰胺 合成 杀菌活性 Thiasporine A 

分 类 号：TQ455.4[化学工程—农药化工]