甘二肽甲酯修饰的新型4-酰基吡唑啉酮衍生物的合成、结构和生物活性  

Synthesis, Structure and Biological Activities of New 1-Phenyl- 3-methyl-4-acyl-2-pyrzolin-5-one Derivatives Modified with Glycylglycine Methyl Ester

作　　者：朱华玲[1] 班立桐[2] 石军[1] 陈晨[1] 尉震[1] 

机构地区：[1]天津农学院基础科学系,天津300384 [2]天津农学院农学系,天津300384

出　　处：《有机化学》2013年第12期2631-2636,共6页Chinese Journal of Organic Chemistry

基　　金：国家星火计划(No.2010GA610009);天津农学院科技发展基金(No.2011N06)资助项目~~

摘　　要：合成了4种未见文献报道的甘二肽甲酯修饰的4-酰基吡唑啉酮衍生物,采用紫外、核磁、红外、元素分析对合成的化合物进行了结构表征,采用X射线单晶衍射方法测定了化合物b3的晶体结构,结果表明合成的化合物以烯胺酮式结构存在.采用单片纸碟法测定了化合物对大肠杆菌和枯草芽孢杆菌的抑菌活性,结果表明大部分的合成化合物都有较弱的抑菌活性,且4位是芳基的化合物的抑菌效果较好.采用平皿法测定了化合物对小麦和油菜的除草活性,结果表明化合物对小麦和油菜的生长都有一定的抑制作用,且对油菜的抑制作用更为明显,尤其是对油菜胚根的生长几乎达到完全抑制.Four new 1-phenyl-3-methyl-4-acyl-2-pyrazolin-5-one derivatives modified with glycylglycine methyl ester were synthesized and characterized by UV, 1H NMR, 13C NMR, IR, elemental analysis. The molecular structure of compound b3 was also characterized by single-crystal X-ray diffraction. The analytical results showed that new compounds existed in enamine-ketone forms. The antibacterial activity tests of the compounds at different concentrations against E. cocli and Bacillus subtilis were performed using disc diffusion method. The results indicated that most compounds had weak abilities of inhibiting the growth of the two bacteria, and the inhibiting abilities of 4-aryl compounds were better. The herbicidal activity tests of the compounds against wheat and rape were performed by plate culture method. The results indicated that all compounds had the abilities of inhibiting the growth of the two plants, and the inhibiting abilities of the compounds against rape were better, especially the inhibiting abilities to the growth of rapeseed radicle almost reached completely suppressed.

关 键 词：吡唑啉酮 甘二肽甲酯 结构 生物活性 

分 类 号：S859.79[农业科学—临床兽医学]