含硫醚和砜亞結(jié)構(gòu)的新型芳香酰胺累衍生物的設(shè)計、合成及生物活性
發(fā)布時間:2021-09-03 12:13
近年來,土壤線蟲危害日趨嚴重,然而市場上應(yīng)用的殺線蟲劑品種匱乏且結(jié)構(gòu)單一。氟吡菌酰胺(fuopyram)是德國拜耳公司開發(fā)的琥珀酸脫氫酶抑制劑(SDHI)類殺菌劑,因其高效和作用機制新穎被廣泛用于土壤線蟲的防治。本文以殺菌、殺線蟲劑氟吡菌酰胺為分子骨架,通過引入硫醚和砜亞結(jié)構(gòu),設(shè)計合成了兩個系列的結(jié)構(gòu)新穎的目標化合物,并經(jīng)核磁共振氫譜(1H NMR)、核磁共振碳譜(13C NMR)和高分辨質(zhì)譜(HRMS)表征新結(jié)構(gòu)。經(jīng)生物活性測試發(fā)現(xiàn),與對照藥氟吡菌酰胺相比,大多數(shù)目標化合物在200μg·mL–1濃度下顯示出優(yōu)異的殺線蟲活性,而當濃度降低為100μg·mL–1時,線蟲死亡率大大降低,其中,化合物Ⅰ-11、Ⅱ-6除外。在殺菌活性方面,化合物Ⅰ-9具有優(yōu)異的抑菌率,其分子對接結(jié)果將為高活性殺菌先導化合物的設(shè)計和探索提供重要的理論指導。
【文章來源】:Engineering. 2020,6(05)EISCI
【文章頁數(shù)】:14 頁
【參考文獻】:
期刊論文
[1]Synthesis, nematicidal activity and docking study of novel chromone derivatives containing substituted pyrazole[J]. Wei Li,Jiuhui Li,Hongfeng Shen,Jiagao Cheng,Zhong Li,Xiaoyong Xu. Chinese Chemical Letters. 2018(06)
[2]新型殺菌劑氟吡菌酰胺的合成[J]. 劉安昌,馮佳麗,賀曉璐,張樹康,余彩虹. 農(nóng)藥. 2015(07)
[3]Synthesis of derivatives of imidazo[4,5-b]pyridine:Novel sulfur contained side chains for macrolide antibiotics[J]. Lu Liu Peng Xu Liang Zhou Ping Sheng Lei~* Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine,Ministry of Education,Institute of Materia Medica,Peking Union Medical College & Chinese Academy of Medical Science,Beijing 100050,China. Chinese Chemical Letters. 2008(01)
本文編號:3381092
【文章來源】:Engineering. 2020,6(05)EISCI
【文章頁數(shù)】:14 頁
【參考文獻】:
期刊論文
[1]Synthesis, nematicidal activity and docking study of novel chromone derivatives containing substituted pyrazole[J]. Wei Li,Jiuhui Li,Hongfeng Shen,Jiagao Cheng,Zhong Li,Xiaoyong Xu. Chinese Chemical Letters. 2018(06)
[2]新型殺菌劑氟吡菌酰胺的合成[J]. 劉安昌,馮佳麗,賀曉璐,張樹康,余彩虹. 農(nóng)藥. 2015(07)
[3]Synthesis of derivatives of imidazo[4,5-b]pyridine:Novel sulfur contained side chains for macrolide antibiotics[J]. Lu Liu Peng Xu Liang Zhou Ping Sheng Lei~* Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine,Ministry of Education,Institute of Materia Medica,Peking Union Medical College & Chinese Academy of Medical Science,Beijing 100050,China. Chinese Chemical Letters. 2008(01)
本文編號:3381092
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