脱氢枞基含氮衍生物的抑菌活性研究

Antibacterial Activity of Dehydroabietyl Nitrogen Derivatives

采用平板计数法研究了脱氢枞酸(1)和脱氢枞基含氮衍生物(脱氢枞胺(2)、脱氢枞酸酰胺衍生物(3a^3m)、脱氢枞胺(取代)苯甲醛Schiff碱衍生物(4a^4i))对6种病原真菌的抑制活性。结果表明:脱氢枞胺的抑菌活性优于脱氢枞酸,脱氢枞胺(取代)苯甲醛Schiff碱衍生物的抑菌活性优于脱氢枞酸酰胺衍生物。其中含卤原子的脱氢枞胺(对氯)水杨醛Schiff碱(4d)、脱氢枞胺(间氟)苯甲醛Schiff碱(4f)、脱氢枞胺(对氟)苯甲醛Schiff碱(4g)、脱氢枞胺(对氯)苯甲醛Schiff碱(4h)具有较强的抑菌活性,4h在质量浓度为180 mg/L时对灰葡萄孢、腐皮镰孢和芸苔链格孢的抑制率达100%,抑制率接近阳性对照物放线菌酮。进一步测定了脱氢枞胺(取代)苯甲醛Schiff碱衍生物4d、4f、4g和4h在不同质量浓度下对6种病原真菌的抑菌活性。结果发现4种化合物在不同质量浓度下对灰葡萄孢和芸苔链格孢均具有较好的抑制活性。化合物4f在22.5 mg/L时对6种病原真菌的抑制率最高,均大于95%,而4g在22.5 mg/L时的抑制率却最低,并且4h在45 mg/L时的抑制率较高,上述结果表明苯环上卤原子的取代位置和类型均会影响其在不同质量浓度下的抑菌活性和最佳抑菌活性的质量浓度。

The antibacterial activities of dehydroabietic acid(1),dehydroabietylamine(2),dehydroabietamide derivatives(3a-3m),dehydroabietylamine benzaldehyde Schiff base derivatives(4a-4i),against six different pathogenic fungi were studied by using plate counting method.The results showed the antibacterial activity of dehydroabietylamine was better than that of dehydroabietic acid,and the antibacterial activities of dehydroabietylamine benzaldehyde Schiff base derivatives were better than that of dehydroabietamide.And the dehydroabietylamine p-chlorosalicylaldehyde Schiff base(4d),dehydroabietylamine m-fluorobenzaldehyde Schiff base(4f),dehydroabietylamine p-fluorobenzaldehyde Schiff base(4g)and dehydroabietylamine p-chlorobenzaldehyde Schiff base(4h)showed strong antibacterial activities.The inhibitory rates of sample 4h against Botrytis cinerea,Fusarium solani and Alternaria brassicae at 180 mg/L were up to 100%,which were close to the positive control,Actinomycin.The antibacterial activities of samples 4d,4f,4g and 4h at mass concentrations of 11.25,22.5,45 and 90 mg/L against six different pathogenic fungi were further studied.All the samples showed excellent antibacterial activities against Botrytis cinerea and Alternaria brassicae at different mass concentrations.The inhibitory rates of sample 4f at 22.5 mg/L against six different pathogenic fungi were more than 95%,but the sample 4g at 22.5 mg/L showed the lowest inhibitory rate.And the sample 4h at 45 mg/L showed the highest antibacterial activities.The above results demonstrated that the substitution position and the type of the halogen atom on the benzene ring affected the antibacterial activity at different mass concentrations and the concentration of the optimum antibacterial activity.