【作者】 周圆； 冯江涛； 张莎莎； 贺红武；

【Author】 ZHOU Yuan;FENG Jiang-tao;Zhang Sha-sha;HE Hong-wu;College of Chemistry, Key Laboratory of Pesticide & Chemical Biology, Ministry of Education,Central China Normal University;

【机构】 华中师范大学化学学院农药与化学生物学教育部重点实验室；

【摘要】 [目的]拟通过设计针对微生物丙酮酸脱羧酶（PDHc-E1）的抑制剂来获得具有杀菌活性的化合物。[方法]通过醛与肼的缩合反应合成了系列新型2,6-二取代-4-氨基嘧啶衍生物I。[结果]发现I系列对E.coli PDHc-E1显示优异的抑制活性。其中I-2对桃核腐病菌的抑制活性(EC₅₀=0.25μM)分别比对照药克菌丹(EC₅₀=95.0μM)和百菌清(EC₅₀=2.11μM)高出380倍和8倍。I-5对两种藻类的抑制活性(EC₅₀=1.4和1.6μM)与硫酸铜(EC₅₀=1.8和1.5μM)相当。[结论]通过对先导结构L1进行结构修饰获得了对E.coli PDHc-E1具有抑制作用的高效杀菌和杀藻活性的化合物。更多还原

【Abstract】 [Aims]This research aims to obtain microbicides with bactericidal activity by designing inhibitors against microbial pyruvate decarboxylase（PDHc-E1）.[Methods]A series of novel2,6-dimethyl-4-aminopyrimidine derivatives I was synthesized by condensation of aldehydes and hydrazine.[Results]All I exhibited potent inhibitory activity against E.coli PDHc-E1.The inhibitory activity of 1-2 against Monilia fructigena(EC₅₀=0.25μM)was 380 times and 8 times higher than that of captan(EC₅₀=95.0 μM)and chlorothalonil(EC₅₀=2.11 μM)respectively.The inhibitory activity of 1-5 against two kinds of algae（EC50=1.4μM and 1.6μM）was similar to that of copper sulfate（EC50=1.8 and 1.5μM）.[Conclusions]The compounds as PDHc-E1 Inhibitors with high antifungal efficiency and algicidal activity were obtained by optimizing the lead structure L1.更多还原