吡唑芳酰基硫脲类衍生物的合成及除草活性评价  

Synthesis and herbicidal activity evaluation of pyrazole arylthioureas derivatives

作　　者：任达 王佳颖 李晓天 刘泓怡 孙素素 陈来 张金林[1] REN Da;WANG Jiaying;LI Xiaotian;LIU Hongyi;SUN Susu;CHEN Lai;ZHANG Jinlin(College of Plant Protection,Hebei Agricultural University,Baoding 071001,China)

机构地区：[1]河北农业大学植物保护学院,河北保定071001

出　　处：《河北农业大学学报》2021年第5期79-84,共6页Journal of Hebei Agricultural University

基　　金：国家自然科学基金资助项目(31871981、32001927);河北省二期现代农业工业技术体系创新团队(hb2018020205).

摘　　要：为发现新型具有除草活性的吡唑芳酰基硫脲类化合物,本研究通过芳酰基异硫氰酸酯和1-甲基-5-氨基吡唑进行缩合,设计合成了一系列共计8个吡唑芳酰基硫脲类衍生物,化合物的结构均经^(1)H NMR、^(13)C NMR和HRMS确证。同时采用小杯法与茎叶处理法对目标化合物的除草活性进行评价,结果表明,在小杯法中,化合物浓度为200 mg/L时,化合物4-2对油菜根长抑制率为87%,对马唐根长和茎长抑制率分别为65%和61%,均显著优于阳性对照药剂莠去津。在茎叶喷雾法,200 mg/L浓度时,化合物4-5对马唐和油菜鲜重抑制率为51%和52%,显著优于阳性对照药剂莠去津。综上,化合物4-2和4-5表现出了相对较好的除草活性,值得进一步研究。In order to discover novel herbicidal activity pyrazole arylthioureas,a series of eight pyrazole aroylthioureas derivatives were designed and synthesized by the condensation reaction of aroyl isothiocyanate and 1-methyl-5-aminopyrazole,and their structures were characterized by^(1)H NMR,^(13)CNMR and HRMS.At the same time,the herbicidal activity of the target compound was evaluated by small cup method and stem and leaf treatment method.The results showed that,with the concentration of 200 mg/L in the small cup method,compound 4-2 displayed 87%inhibition against the rape root length,and the inhibition rates of root length and stem length were 65%and 61%respectively,which were significantly better than that of the positive control atrazine.With the concentration of 200 mg/L in the stem and leaf spray method,compound 4-5 exhibited moderate herbicidal activities against crabgrass and rape fresh weight with inhibition values of 51%and 52%,which was significantly better than that of the positive control atrazine.In conclusion,it indicated that compounds 4-2 and 4-5 displayed good herbicidal activities,which was worthy of further study.

关 键 词：吡唑芳酰基硫脲 设计 化学合成 除草活性 

分 类 号：S482.1[农业科学—农药学]