3-对■烯-1-胺及其席夫碱衍生物的抑菌活性研究

Antimicrobial Activities of p-Menth-3-en-1-amine and Its Schiff Base Derivatives

利用微量肉汤稀释法测定3-对[艹孟]烯-1-胺(1)及其席夫碱衍生物(2a^2l)对革兰氏阳性菌金黄色葡萄球菌、革兰氏阴性菌肺炎克雷伯氏菌及真菌白色念珠菌的抑菌活性,并讨论了构效关系。结果表明:3-对[艹孟]烯-1-胺及其部分席夫碱衍生物对这3种菌具有一定的抑菌活性,其中化合物1对金黄色葡萄球菌的抑菌活性最强,最小抑菌浓度(MIC)值为56.25mg/L;化合物2h和2i对肺炎克雷伯氏菌的抑菌活性最强,MIC值均为112.5mg/L;化合物2l对白色念珠菌的抑菌活性最强,MIC值为28.125mg/L。构效关系分析结果表明:向3-对[艹孟]烯-1-胺席夫碱衍生物中引入Br、Cl等卤素后,能显著增强抑菌活性;含有吡啶环的3-对[艹孟]烯-1-胺席夫碱衍生物对真菌白色念珠菌的抑菌活性明显要高于含呋喃环、吡咯环或噻吩环的3-对[艹孟]烯-1-胺席夫碱衍生物。

The antimicrobial activities of p -menth-3-en-1-amine (1) and its Schiff base derivatives (2a - 2l) against Staphylococcus aureus (gram-positive bacteria),Klebsiella pneumonia (gram-negative bacterium) and Candida albicans (fungus) were measured by using the microbroth dilution method.Then,the structure-activity relationship was established.The results showed that some products had certain antibacterial activities against these pathogenic bacteria.Compound 1 had the strongest antimicrobial activity against Staphylococcus aureus and the minimal inhibitory concentration(MIC) was 56.25 mg/L.Compound 2h and 2i had the strongest antimicrobial activity against Klebsiella pneumonia and the MICs were 112.5 mg/L.Compounds 2l had the strongest antimicrobial activities against Candida albicans and the MIC was 28.125 mg/L.The structure-activity relationship indicated that the antimicrobial activity would be stronger when the chlorine or bromine atom was introduced into the Schiff base derivatives;the antimicrobial activities of Schiff base derivatives containing a pyridine ring were higher than those of the Schiff base derivatives containing a furan,pyrrole or thiophene.