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将取代黄酮醇引入亚磷酸二乙酯,设计合成了14个含取代黄酮基磷酸酯类新化合物,通过1H NMR,13C NMR,31P NMR,MS,IR和HRMS对它们的结构进行了表征.采用浊度法测试了目标化合物的离体抑菌活性,表明部分目标化合物在100μg/m L浓度下对水稻白叶枯病菌表现出良好的抑制率,明显优于对照药剂噻菌铜和叶枯唑(≥57.4%).其中O,O’-二乙基-O’’-(2’,7-二甲氧基黄酮-3-基)磷酸酯(2b)、O,O’-二乙基-O’’-(2’-甲氧基-7-乙氧基黄酮-3-基)磷酸酯(2f)和O,O’-二乙基-O’’-(3’,4’-二甲氧基-7-乙氧基黄酮-3-基)磷酸酯(2m)在100μg/m L浓度下对水稻白叶枯病菌的抑制率分别达到92.8%,87.7%和88.3%.O,O’-二乙基-O’’-(4’-氟-7-乙氧基黄酮-3-基)磷酸酯(2h)和O,O’-二乙基-O’’-(4’-甲基-7-乙氧基黄酮-3-基)磷酸酯(2k)在100μg/m L浓度下对柑橘溃疡病菌也有较好的抑制活性,其抑制率分别为85.1%和71.7%.
Fourteen flavonoid-containing phosphates were designed and synthesized by replacing the flavonol with diethyl phosphite, and their structures were characterized by 1H NMR, 13C NMR, 31P NMR, MS, IR and HRMS. The in vitro antibacterial activities of the target compounds were tested by turbidity method, indicating that some of the target compounds showed good inhibitory rates against the bacterial leaf blight at a concentration of 100 μg / mL, which was significantly better than that of the control agents thiabendazole and metoxazole (≧ 57.4%) wherein O, O’-diethyl-O “- (2 ’, 7-dimethoxyflavone- 3-yl) phosphate -O’’- (2’-methoxy-7-ethoxyflavone-3-yl) phosphate and O, Dimethoxy-7-ethoxyflavone-3-yl) phosphate (2m) reached 92.8%, 87.7% and 88.3%, respectively, at the concentration of 100μg / (4’-fluoro-7-ethoxyflavone-3-yl) phosphate (2h) and O, O’-diethyl-O ” -methyl-7-ethoxyflavone-3-yl) phosphate (2k) had a good inhibitory activity against citrus canker at a concentration of 100μg / mL with the inhibitory rates of 85.1% and 71.7%, respectively.