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(jì)、合成及生物活性
發(fā)布時(shí)間:2021-09-03 12:13
近年來(lái),土壤線蟲(chóng)危害日趨嚴(yán)重,然而市場(chǎng)上應(yīng)用的殺線蟲(chóng)劑品種匱乏且結(jié)構(gòu)單一。氟吡菌酰胺(fuopyram)是德國(guó)拜耳公司開(kāi)發(fā)的琥珀酸脫氫酶抑制劑(SDHI)類(lèi)殺菌劑,因其高效和作用機(jī)制新穎被廣泛用于土壤線蟲(chóng)的防治。本文以殺菌、殺線蟲(chóng)劑氟吡菌酰胺為分子骨架,通過(guò)引入硫醚和砜亞結(jié)構(gòu),設(shè)計(jì)合成了兩個(gè)系列的結(jié)構(gòu)新穎的目標(biāo)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(cè)試發(fā)現(xiàn),與對(duì)照藥氟吡菌酰胺相比,大多數(shù)目標(biāo)化合物在200μg·mL–1濃度下顯示出優(yōu)異的殺線蟲(chóng)活性,而當(dāng)濃度降低為100μg·mL–1時(shí),線蟲(chóng)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(duì)接結(jié)果將為高活性殺菌先導(dǎo)化合物的設(shè)計(jì)和探索提供重要的理論指導(dǎo)。
【文章來(lái)源】:Engineering. 2020,6(05)EISCI
【文章頁(yè)數(shù)】:14 頁(yè)
【參考文獻(xiàn)】:
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(shù)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(hào):3381092
【文章來(lái)源】:Engineering. 2020,6(05)EISCI
【文章頁(yè)數(shù)】:14 頁(yè)
【參考文獻(xiàn)】:
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(shù)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(hào):3381092
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