5-氯水杨醛缩2,4-二羟基苯酰肼的合成及其抗菌活性的研究  

The synthesis of 2,4-dihydroxy-N'-(5-chloro-2-hydroxybenzylidene and its antibacterial activity

作　　者：黄珊珊[1] 袁汝强 刁云鹏[1] 李倩[1] 张宝璟[1] 甄宇红[1] 张厚利[1] 

机构地区：[1]大连医科大学药学院,辽宁大连116044

出　　处：《中国微生态学杂志》2013年第12期1379-1382,共4页Chinese Journal of Microecology

摘　　要：目的合成5-氯水杨醛缩2,4-二羟基苯酰肼,对其进行结构表征,并测定其抑菌活性。方法运用席夫碱合成原理,合成目标产物,通过单晶衍射分析确定其分子结构。采用试管法和平板法测定其对肺炎克雷伯杆菌MIC,MBC,绘制杀菌曲线,并通过透射电镜研究其作用机制。结果成功合成目标化合物,通过单晶衍射分析确定为5-氯水杨醛缩2,4-二羟基苯酰肼。抗菌结果表明该化合物对肺炎克雷伯菌的MIC为1.25 mg/mL,MBC为2.5 mg/mL。杀菌曲线结果表明该化合物对肺炎克雷伯菌的杀菌作用表现出明显的浓度依赖性。电镜结果表明该化合物的作用机制可能与破坏菌体细胞壁,改变细胞膜通透性有关。结论产物5-氯水杨醛缩2,4-二羟基苯酰肼有较好的抗肺炎克雷伯杆菌的作用。Objective To synthesis 2,4-dihydroxy-N＇- （5-chloro-2-hydroxybenzylidene） benzohydrazide, and characterize the structure, and to test the antibacterial activities of this compound in vitro. Methods According to the synthesis principle of Schiff base, the target product was synthesized, single-crystal X-ray diffraction was used to analyze its molecular structure. Antibacterial activities of the compounds on Klebsiella pneumonia was screened by tube method. The results were evaluated by MIC value, MBC value, and the killing curve. The mechanisms of in- hibition were studied by transmission electron microscopy. Results The novel compound of 2,4-dihydroxy-N＇-（5- chloro-2-hydroxybenzylidene） benzohydrazide was synthesized successfully and the structure was confirmed by single-crystal X-ray diffraction. The MIC and MBC of the compound were 1.25 mg/mL and 2. 5 mg/mL. The killing curve showed the bactericidal action had a concentration-dependent. Transmission electron microscopy results show that the mechanism of action of the compound may destroy bacterial cell walls, changing the permeability of the cell membrane. Conclusion The target compound was synthesized correctly. 2,4-dihydroxy-N＇-（ 5-chloro-2-hydroxy- benzylidene） had significant antibacterial effect on Klebsiella pneumonia.

关 键 词：5-氯水杨醛缩2 4-二羟基苯酰肼 合成 抗菌 

分 类 号：R378.991[医药卫生—病原生物学]