Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Eur J Med Chem. 2010 Aug;45(8):3293-8. doi: 10.1016/j.ejmech.2010.04.012. Epub 2010 Apr 18.
In this study 12 novel benzimidazole compounds bearing hydrazone moiety were synthesized in order to investigate their possible antibacterial and antifungal activity. Structures of the synthesized compounds were elucidated by spectral data. Six different gram-negative and four different gram-positive bacterial strains were used in antibacterial activity tests. Antifungal activity tests were also performed against three different fungal strains. Most of the test compounds found to be significantly effective against Proteus vulgaris, Staphylococcus typhimurium, Klebsiella pneumoniae and Pseudomonas aeruginosa gram-negative bacterial strains. A structure-activity relationship (SAR) study including some electronic parameters was carried out and a connection between antibacterial activity and electronic properties of the target compounds was determined. Toxicity of the most effective compounds was established by performing Brine-Shrimp lethality assay.
在这项研究中，合成了 12 种含有腙部分的新型苯并咪唑化合物，以研究它们可能的抗菌和抗真菌活性。通过光谱数据阐明了合成化合物的结构。在抗菌活性测试中使用了六种不同的革兰氏阴性菌和四种不同的革兰氏阳性菌。还对三种不同的真菌菌株进行了抗真菌活性测试。大多数测试化合物对革兰氏阴性菌变形杆菌、鼠伤寒沙门氏菌、肺炎克雷伯菌和铜绿假单胞菌具有显著的抑制活性。进行了包括一些电子参数的构效关系 (SAR) 研究，并确定了抗菌活性与目标化合物电子性质之间的关系。通过进行盐水虾致死试验来确定最有效的化合物的毒性。
