Ertan Tugba, Yildiz Ilkay, Ozkan Semiha, Temiz-Arpaci Ozlem, Kaynak Fatma, Yalcin Ismail, Aki-Sener Esin, Abbasoglu Ufuk
Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Tandogan, Ankara, Turkey.
Bioorg Med Chem. 2007 Mar 1;15(5):2032-44. doi: 10.1016/j.bmc.2006.12.035. Epub 2006 Dec 24.
A new series of N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamide and phenylacetamide derivatives (1a-1n, 2a-2n) were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Candida albicans, and their drug-resistant isolate. Microbiological results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms at MIC values between 500 and 1.95 microg/ml. Benzamide derivative 1d exhibited the greatest activity with MIC values of 1.95, 3.9, and 7.8 microg/ml against drug-resistant B. subtilis, B. subtilis, and S. aureus, respectively.
合成了一系列新的N-(2-羟基-4(或5)-硝基/氨基苯基)苯甲酰胺和苯乙酰胺衍生物(1a-1n, 2a-2n),并对其针对金黄色葡萄球菌、枯草芽孢杆菌、肺炎克雷伯菌、铜绿假单胞菌、大肠杆菌、白色念珠菌及其耐药菌株的抗菌和抗真菌活性进行了评估。微生物学结果表明,这些化合物对测试微生物具有广谱活性,MIC值在500至1.95微克/毫升之间。苯甲酰胺衍生物1d表现出最大活性,对耐药枯草芽孢杆菌、枯草芽孢杆菌和金黄色葡萄球菌的MIC值分别为1.95、3.9和7.8微克/毫升。