摘要
为了寻求新的含吡唑双杂环先导化合物,用 4 取代 1 甲基 3 乙基 5 吡唑甲酰氯与 3 甲基 5 吡唑酮、3 乙基 5 吡唑甲酸乙酯等含氮杂环反应得到了 8个新的含吡唑环的双杂环类化合物。经IR、1HNMR、MS和元素分析对化合物的结构进行了表征。初步生物活性实验结果表明:在25μg/mL浓度下,5d对水稻稻瘟病菌Pyriculariaoryzae的抑制率为 45.6%;在 500μg/mL浓度下,5c对稻黑尾叶蝉Nephotettixcincticeps的死亡率为 53.9%。
In order to search for the new pyrazolyl-heterocycles lead compounds, eight pyrazolyl-(heterocycles) were synthesized from 3-ethyl-1-methyl- 4-substituted-5-pyrazolecarboxylic acid chloride and nitrogen heterocyclic rings such as 3-methyl-5-pyrazolone, 1H-3-ethyl-5-pyrazole (carboxylic) (ethyl) ester, etc. The structures of the new compounds were confirmed by ^(1)H NMR, IR, MS and (elementary) analysis. The results of pretiminary biological tests indicated that compound 5d showed (inhibitory) activities (45.6%) against Pyricularia oryzae at 25 μg/mL. 5c showed inhibitory (activities) (53.9%) against Nephotettix cincticeps at (500 μg/mL.)
出处
《农药学学报》
CAS
CSCD
2005年第1期69-72,共4页
Chinese Journal of Pesticide Science
基金
浙江省教育厅资助项目(20030145).
关键词
吡唑
双杂环
含氮杂环
生物活性
pyrazole
bis-heterocycles
nitrogen heterocyclic rings
biological activity
