啶酰菌胺类似物的合成及抑菌活性

Synthesis and antifungal activity of novel analogs of boscalid

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50 μg/mL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58.86 μg/mL，总体活性与啶酰菌胺相当，具有进一步研究的价值。

Abstract: 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, 13C NMR and HRMS. The preliminary results showed that most of the compounds possessed some fungicidal activity to seven phytopathogenic fungi at 50 μg/mL. 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/mL, respectively.