N-取代苯基-5-三氟甲基-4-吡唑酰胺类化合物的合成及抗植物真菌生物活性研究  

Synthesis and Antifungal Activity Studies of N-(Substituted Phenyl)-5-Trifluoromethyl-1 H-Pyrazole-4-Carboxamide Derivatives

作　　者：吴志兵[1,2] 牛雪 杨晶欣 谢德文 张承志 WU Zhibing;NIU Xue;YANG Jingxin;XIE Dewen;ZHANG Chengzhi(State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering,Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Guizhou University,Guiyang 550025,China;Center for R&D of Fine Chemicals of Guizhou University,Guiyang 550025,China;School of Chemistry and Chemical Engineering,Guizhou University,Guiyang 550025,China;College of Pharmacy,Guizhou University,Guiyang 550025,China)

机构地区：[1]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,教育部绿色农药与生物工程重点实验室,贵州贵阳550025 [2]贵州大学精细化工研究开发中心,贵州贵阳550025 [3]贵州大学化工学院,贵州贵阳550025 [4]贵州大学药学院,贵州贵阳550025

出　　处：《贵州大学学报（自然科学版）》2021年第5期44-49,共6页Journal of Guizhou University:Natural Sciences

基　　金：贵州省科技计划资助项目(黔科合成果[2017]4108);贵州大学培育资助项目(贵大培育[2019]31号)。

摘　　要：吡唑酰胺类化合物是一类具有独特作用机制的化合物,为了发现更高活性的吡唑酰胺类化合物,设计并合成了9个结构新颖的N-取代苯基-5-三氟甲基-4-吡唑酰胺类化合物。采用生长速率法,测试了化合物对5种植物病原真菌:小麦赤霉病菌(Fusarium graminearum)、辣椒枯萎病菌(Fusarium oxysporum)、茄子黄萎病菌(Verticillium dahliae)、水稻纹枯病菌(Thanatephorus cucumeris)和油菜菌核病菌(Sclerotinia sclerotiorum)的抑制活性。初步生物活性表明:在100μg/mL浓度下,部分目标化合物对测试真菌有一定的抑制作用,其中化合物5d对茄子黄萎病菌和水稻纹枯病菌的抑制率分别为51.5%和65.8%,为进一步结构优化提供参考。Pyrazole carboxamide is a series of compounds with a unique mechanism of action.In order to discover higher activity compounds,nine novel N-substituted-1-phenyl-5-trifluoromethyl-1 H-pyrazole-4-carboxamide derivatives were designed and synthesized.Antifungal activity of all the target compounds were tested using the growth rate method against five plant pathogenic fungi:Fusarium graminearum,Fusarium oxysporum,Verticillium dahliae,Thanatephorus cucumeris and Sclerotinia sclerotiorum.Preliminary biological activity results revealed that some target compounds exhibited a certain inhibitory on the tested fungi at a concentration of 100μg/mL.Among them,the inhibition rates of 5d against Verticillium dahliae and Thanatephorus cucumeris were 51.5% and 65.8%,respectively,which providing some supports for further structural optimization.

关 键 词：吡唑酰胺 合成 抗真菌活性 

分 类 号：TQ450.21[化学工程—农药化工]