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
收稿日期: 2013-06-17
修回日期: 2013-07-17
网络出版日期: 2013-08-12
基金资助
国家星火计划(No. 2010GA610009)和天津农学院科技发展基金(No. 2011N06)资助项目.
Synthesis, Structure and Biological Activities of New 1-Phenyl-3-methyl-4-acyl-2-pyrzolin-5-one Derivatives Modified with Glycylglycine Methyl Ester
Received date: 2013-06-17
Revised date: 2013-07-17
Online published: 2013-08-12
Supported by
Project supported by the China Spark Program (No. 2010GA610009) and the Science Development Fund of Tianjin Agricultural College (No. 2011N06).
朱华玲 , 班立桐 , 石军 , 陈晨 , 尉震 . 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[J]. 有机化学, 2013 , 33(12) : 2631 -2636 . DOI: 10.6023/cjoc201306021
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.
Key words： pyrazolotone; glycylglycine ester; structure; biological activity
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