N-芳基氨基甲酸苄酯的合成及抗真菌活性研究

Synthesis and Antifungal Activity of N-Arylaminomethyl Benzyl Ester

为发现更多抗真菌药物分子,设计合成16种N-芳基氨基甲酸苄酯类目标化合物,并进行结构鉴定;以醚菌酯为阳性对照,采用菌丝线性生长速率法,测定目标化合物对常见的10种植物病原真菌的体外抑制活性,以及5种高抗菌活性的目标化合物对苹果轮纹病原菌和番茄早疫病原菌的毒力。结果发现,所有目标化合物对10种供试真菌都有不同程度的抑制活性,其中,化合物B11抗菌活性最高,对9种供试真菌的抑制率均超过80%,对马铃薯干腐病原菌的抑制率为98.1%,对番茄早疫病原菌的EC50为7.6μg/mL。构效关系研究表明,-F和-Me的引入有利于提高活性,是该类化合物的优势基团;-F和-Me的组合可大幅度提高活性,是优势基团叠加效应的结果。

To discover novel antifungal molecules,we designed and synthesized 16 target compounds of N-arylaminomethyl benzyl esters and identified their structures.With kresoxim-methyl as the positive control,the inhibitory effects of the target compounds on 10 common phytopathogenic fungi were determined by the mycelial growth rate method.Furthermore,the toxicity of 5 highly antifungal target compounds to Botryosphaeria dothidea and Alternaria solani was determined.The results showed that all the target compounds inhibited the growth of the 10 tested fungi.Among them,compound B11 had the highest antifungal activity,with the inhibition rates over 80%against 9 tested fungi.In addition,compound B11 demonstrated the inhibition rate of 98.1%against Fusarium sambucinum and the EC50 of 7.6μg/mL against A.solani.The analysis of structure-activity relationship showed that-F and-Me increased the compound activity,being the dominant functional groups of such compounds.The combination of-F and-Me significantly enhanced the compound activity,which was attributed to the combined effect of dominant functional groups.