Erol D D, Calis U, Yuluğ N
Pharmaceutical Chemistry Department, Hacettepe University, Ankara, Turkey.
Arzneimittelforschung. 1996 Feb;46(2):205-6.
A number of 3-(4-substituted benzoyl methyl)-2-benzoxazolinones have been synthesized by reacting with 2-benzoxazolinone and 4-substitutet phenacyl bromide in ethanol. Their structures were confirmed by microanalysis, IR and NMR spectral analysis. Possible antimicrobial activity of the compounds was investigated by tube dilution and paper disc techniques using bacteria (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus faecalis RSKK 10541) and yeast-like fungi (Candida parapsilosis, Candida albicans, Candida pseudotropicalis, Candida stellaoidea). Among the compounds tested 3-(4-bromo benzoylmethyl)-5-chloro-2-benzoxazolinone (compound 4) and 3-(4-nitro benzoyl methyl)-5-chloro-2-benzoxazolinone (compound 6) showed the most favorable activity.
通过2-苯并恶唑啉酮与4-取代苯甲酰甲基溴在乙醇中反应，合成了一系列3-(4-取代苯甲酰甲基)-2-苯并恶唑啉酮。通过微量分析、红外光谱和核磁共振光谱分析确定了它们的结构。采用试管稀释法和纸片法，以细菌（大肠埃希菌ATCC 25922、金黄色葡萄球菌ATCC 25923、铜绿假单胞菌ATCC 27853、粪肠球菌RSKK 10541）和酵母样真菌（近平滑念珠菌、白色念珠菌、伪热带念珠菌、星状念珠菌）为受试对象，研究了这些化合物可能具有的抗菌活性。在所测试的化合物中，3-(4-溴苯甲酰甲基)-5-氯-2-苯并恶唑啉酮（化合物4）和3-(4-硝基苯甲酰甲基)-5-氯-2-苯并恶唑啉酮（化合物6）表现出最良好的活性。
