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Position: Home > Articles > Synthesis and antifungal activity of novel analogs of boscalid Chinese Journal of Pesticide Science 2016,18 (4) 424-430

啶酰菌胺类似物的合成及抑菌活性

作  者:
杜士杰;覃兆海
单  位:
铜仁学院材料与化学工程学院;中国农业大学理学院
关键词:
啶酰菌胺;酰胺;抑菌活性;琥珀酸脱氢酶抑制剂
摘  要:
为了筛选具有更高杀菌活性的化合物,在啶酰菌胺结构的基础上,设计合成了2个系列共计21个新的2-氯烟酰胺类化合物(3a~3h,5a~5n),其结构均通过核磁共振氢谱、碳谱及高分辨质谱确认。离体杀菌活性测定结果表明,在50μg/m L下,多数目标化合物对供试7种病原菌表现出一定的抑制活性,其中化合物3h对西瓜炭疽病菌Colletotrichum orbiculare和番茄灰霉病菌Botrytis cinerea的抑制率分别为94.1%和95.6%。精密毒力测定表明,3h对棉花立枯丝核菌Rhizoctonia solani、西瓜炭疽病菌和番茄晚疫病菌Phytophthora infestans的EC50值分别为4.56、14.35和58.86μg/m L,总体活性与啶酰菌胺相当,具有进一步研究的价值。
译  名:
Synthesis and antifungal activity of novel analogs of boscalid
作  者:
DU Shijie;QIN Zhaohai;College of Material and Chemical Engineering, Tongren University;College of Science, China Agricultural University;
关键词:
boscalid;;amide;;fungicidal activity;;succinate dehydrogenase inhibitors
摘  要:
A series of novel 2-chloro-nicotinamides(3a-3h, 5a-5n) were designed and synthesized based on the lead compound boscalid. The structures were characterized by 1H NMR, 13 C NMR and HRMS. The preliminary results showed that most of the compounds possessed some fungicidal activity to seven phytopathogenic fungi at 50 μg/m L. Notably, compound 3h showed similar fungicidal activity and the broadest spectrum as boscalid. It exhibited the inhibition rate of 94.1% and 95.6% to the Colletotrichum orbiculare and Botrytis cinerea, respectively and the EC50 value against Rhizoctonia solani, C. orbiculare and Phytophthora infestans was 4.56,14.35 and 58.86 μg/m L, respectively.

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