含硝基胍的亚砜亚胺衍生物的设计、合成和抑菌活性研究

Study on the design,synthesis,and antifungal activity of sulfoximine derivatives containing nitroguanidine motif

本文通过活性亚结构连接方法,把硝基胍和硫醚通过氧化、偶联连接起来,设计合成了一系列亚砜亚胺类化合物,并对六种病原菌进行了抑菌活性测试。结果表明,大多数化合物具有一定的抑菌活性,化合物6c显示出广谱的抑菌活性,在50μg·mL^(-1)对油菜菌核菌、辣椒疫霉菌、番茄灰霉菌、禾谷镰刀菌、水稻纹枯菌和稻瘟菌的抑制率分别为75.7%、49.4%、56.6%、48.0%、60.6%、57.4%。

A series of sulfoximine derivatives were designed and synthesized by the oxidation coupling reaction of sulfides and N-alkyl nitroguanidines using the principle of substructure splicing in this paper,and the fungicidal activities of the target compounds against six fungi were evaluated.The results showed that most of the compounds exhibited antifungal activity.Among them,compound 6c displayed a broad spectrum of fungicidal activity in vitro with an inhibition rate of 75.7%、49.4%,56.6%,48.0%,60.6% and 57.4% against Sclerotinia sclerotiorum,Phytophthora capsici,Botrytis cinerea,Fusarium graminearum,Rhizoctonia solani,and Pyricularia grisea,respectively.