新型含氮化合物对柑桔绿霉菌的离体抑菌活性及其构效关系

为寻找对柑桔绿霉菌具有抑制作用的活性化合物,采用生长速率法并结合光谱法评价两种商品化三唑类杀真菌剂和四种新型含氮化合物对柑桔绿霉菌的抑菌活性及与柑桔绿霉菌CYP51的结合能力。结果表明:7-甲氧基-2-氢-苯并[b][1,4]噻嗪-3-胺对柑桔绿霉菌表现出强抑制作用,EC50值达1.18mg/L,与商品化三唑类杀真菌剂烯唑醇的EC50值(0.09mg/L)接近;而其余三种新型含氮化合物显示出中等程度的抑制作用,EC50值分别为7.88、10.09和38.56mg/L。不同化合物与异源表达的重组柑桔绿霉菌CYP51的结合能力不同,对柑桔绿霉菌生长抑制的EC50越大,结合常数越大,即化合物与靶标酶CYP51的结合能力与抑菌活性呈正相关。

The antifungal activities of different new nitrogen compounds against Penicillium digitatum and their structure-activity relationships

To identify and select the active compounds which have antifungal activities on Penicillium digitatum,the growth rate and the binding-spectroscopic analysis was used to evaluate the antifungal activities and the binding capacity of fungicide with P.digitatum CYP51 about two triazole fungicides and four new nitrogen compounds.The results showed that 7-methoxy-2H-benzo[b][1,4]thiazin-3-amine displayed strong antifungal property,and the EC 50 was 1.18 mg/L which was close to the diniconazole(0.09 mg/L);and moderate antifungal effects were observed with the other three nitrogen compounds with the EC 50 of 7.88,10.09,38.56 mg/L,respectively.Different compounds had different binding capacities with heterologous expression of CYP51 in citrus green mold.There is a positive correlation between antibacterial activity of compounds and the ability of compounds combined with CYP51.Analysis of structure-activity relationship showed that the introduction of sulfur may increase the capacity of compounds to suppression of green mold.