| 摘要: |
| 【目的】合成高活性的(E)-2-甲氧亚胺基-2-［2-(2-氧代喹啉-4-氧甲基)苯基］乙酸甲酯类化合物，为以后优化和设计新化合物提供理论依据。【方法】以（E）-2-甲氧亚胺基-2-［2′-(溴甲基)苯基］乙酸甲酯和4-羟基喹啉-2-酮类化合物为原料，通过醚化反应，合成了10a～10k等11种(E)-2-甲氧亚胺基-2-［2-(2-氧代喹啉-4-氧甲基)苯基］乙酸甲酯类化合物，对其进行ESI-MS、IR谱及1H NMR谱分析。以嘧菌酯为对照，采用生长速率法测定化合物10a～10k对烟草赤星病菌、棉花枯萎病菌、水稻瘟疫病菌、玉米弯孢病菌、番茄早疫病菌、苹果腐烂病菌的抑菌活性。【结果】合成了11个(E)-2-甲氧亚胺基-2-［2-(2-氧代喹啉-4-氧甲基)苯基］乙酸甲酯类化合物，确认了其结构。除10a和10d外，其他9个化合物在质量浓度为50 mg/L时对6种供试植物病原菌均具有一定的抑菌活性；化合物10a对烟草赤星病菌的抑制率达91.5%，10c对水稻瘟疫病菌的抑制率达93.3%。【结论】合成了11个(E)-2-甲氧亚胺基-2-［2-(2-氧代喹啉-4-氧甲基)苯基］乙酸甲酯类化合物，除个别化合物外均对6种供试病原菌具有较好的抑菌活性。 |
| 关键词: （E）-2-甲氧亚胺基-2-［2′ (溴甲基)苯基］乙酸甲酯 4-羟基喹啉-2-酮 抑菌活性 |
| DOI： |
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| Synthesis and antifungal activity of a class of compounds |
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JIANG Lianrui,TIAN Yangguang,ZHOU Wenming
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| Abstract: |
| 【Objective】The study synthesized the highly active novel methyl (E)-2-(methoxyimino)-2-(2-(((2-oxo-1,2-dihydroquinolin-4-yl)oxy)methyl)phenyl)acetate compounds to provide theoretical basis for optimization and design of new compounds.【Method】 Novel methyl (E)-2- (methoxyimino)-2-(2-(((2-oxo-1,2-dihydroquinolin-4-yl)oxy)methyl)phenyl)acetate compounds named 10a-10k were synthesized from (E)-2-methoxyimino 2-［2′-(methyl bromide)phenyl］ acetate and 4-hydroxy-1,2-dihydroquinolin-2-one by etherification. Growth rate method was used to test the antifungal activities of these compounds against Alternaria alternate,Fusarium oxysporum vasinfectum,Pyricularia Grisea,Curvularia lunata,Alternaria solani,Valsa mali and compared with the antifungal activity of Azoxystrobin.【Result】 Eleven compounds were synthesized and their structures were confirmed by IR,ESI-MS and 1H NMR.When the mass concentration was 50 mg/L,most of the compounds exhibited different inhibiting effect against all the tested strains except 10a and 10d.In particular,the inhibition rate of compound 10a against Alternaria alternata was 91.5% and that of compound 10c against Pyricularia grisea was 93.3%.【Conclusion】A total of 11 novel methyl (E)-2-(methoxyimino)-2-(2-(((2-oxo-1,2-dihydroquinolin-4-yl)oxy) methyl)phenyl)acetate compounds were synthesized and they exhibited good antifungal activities against tested strains. |
| Key words: (E)-2-methoxyimino-2-［2′ (methyl bromide)phenyl］ acetate 4-hydroxy-1,2-dihydroquinolin-2-one antifungal activity |
