Agh-Atabay Naz M, Dulger Basaran, Gucin Fahrettin
Faculty of Arts and Science, Fatih University, 34900 Hadimkoy, Istanbul, Turkey.
Eur J Med Chem. 2003 Oct;38(10):875-81. doi: 10.1016/s0223-5234(03)00146-6.
The 1,2-bis(2-benzimidazyl)-1,2-ethanediol (1), 1,4-bis(2-benzimidazyl)-1,2,3,4-butanetetraol (2), 1,3-bis(2-benzimidazyl)-2-thiapropane (3), 1,3-bis(2-benzimidazyl)-2-thia-propane-dihydrochloride (4), 1,5-bis(2-benzimidazyl)-3-thiapentane (5), and 1,5-bis(2-benzimidazyl)-3-thiapentane dihydrochloride (6) chelating ligands are synthesised and characterised by using analytical data and modem spectroscopic methods such as FT-Raman, FT-IR, 1H- and 13C-NMR spectrometers. Their antimicrobial activities are reported by comparing the in vitro activities, with those of ofloxacin, ciprofloxacin, piperacillin, ampicillin and cefazolin antibacterial agents against fresh clinical isolates. Antifungal activities are reported on Candida albicans, Candida utilis, Cryptococcus neoformans fungi, and the results are referenced with amphotericin-B, fluconazole and flucytosine antifungal agents. It has been found that all the compounds have broad spectra activity and was either more active or equipotent to those compared antibiotic and antifungal agents.
合成了1,2 - 双（2 - 苯并咪唑基）-1,2 - 乙二醇（1）、1,4 - 双（2 - 苯并咪唑基）-1,2,3,4 - 丁四醇（2）、1,3 - 双（2 - 苯并咪唑基）-2 - 硫代丙烷（3）、1,3 - 双（2 - 苯并咪唑基）-2 - 硫代丙烷二盐酸盐（4）、1,5 - 双（2 - 苯并咪唑基）-3 - 硫代戊烷（5）和1,5 - 双（2 - 苯并咪唑基）-3 - 硫代戊烷二盐酸盐（6）等螯合配体，并通过分析数据和傅里叶变换拉曼光谱、傅里叶变换红外光谱、1H - 和13C - 核磁共振光谱仪等现代光谱方法对其进行了表征。通过比较这些化合物与氧氟沙星、环丙沙星、哌拉西林、氨苄西林和头孢唑林等抗菌剂对新鲜临床分离株的体外活性，报道了它们的抗菌活性。还报道了这些化合物对白色念珠菌、产朊假丝酵母、新型隐球菌等真菌的抗真菌活性，并与两性霉素B、氟康唑和氟胞嘧啶等抗真菌剂的结果进行了对比。结果发现，所有这些化合物都具有广谱活性，并且对所比较的抗生素和抗真菌剂而言，要么活性更高，要么效力相当。
