1-(吡唑-5-酰基)-1H-取代吡唑的合成及生物活性

Synthesis of 1H-Substituted 1- pyrazole, and their Biological Activities

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、1H NMR、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25 μg/mL浓度下, 5d 对水稻稻瘟病菌Pyricularia oryzae的抑制率为45.6%;在500 μg/mL浓度下, 5c 对稻黑尾叶蝉Nephotettix cincticeps的死亡率为53.9%。

Abstract: 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 1H 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.