Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Tandogan, Ankara, Turkey.
Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Microbiology, 06330 Etiler, Ankara, Turkey.
Z Naturforsch C J Biosci. 2013 Nov-Dec;68(11-12):453-60.
A new series of 5-(p-substituted benzamido/phenylacetamido)-2-(p-tert-butylphenyl)benzoxazole derivatives were synthesized and evaluated for their antibacterial, antifungal, and antimycobacterial activities against antibiotic-resistant and -sensitive Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, and Mycobacterium tuberculosis as well as against Candida albicans and Candida krusei. The compounds possessed broad-spectrum activity against all of the tested Gram-positive and Gram-negative bacteria and yeasts, their minimum inhibitory concentrations (MICs) ranging between 16-128 microg/ml. One compound exhibited significant antibacterial activity (16 microg/ml) against an antibiotic-resistant Enterococcus faecalis isolate, having twice the potency of the compared standard drugs vancomycin and gentamycin sulfate. The compounds also showed moderate antitubercular activity with MIC values between 8-128 microg/ml against Mycobacterium tuberculosis and its clinical isolate.
合成了一系列新的 5-（对取代苯甲酰胺/苯乙酰胺基）-2-（对叔丁基苯基）苯并恶唑衍生物，并评估了它们对耐抗生素和敏感的金黄色葡萄球菌、粪肠球菌、大肠杆菌、肺炎克雷伯菌和结核分枝杆菌以及白色念珠菌和克柔念珠菌的抗菌、抗真菌和抗分枝杆菌活性。这些化合物对所有测试的革兰氏阳性和革兰氏阴性细菌和酵母具有广谱活性，其最小抑菌浓度（MIC）在 16-128 μg/ml 之间。一种化合物对一种抗抗生素的粪肠球菌分离株表现出显著的抗菌活性（16 μg/ml），其效力是比较标准药物万古霉素和硫酸庆大霉素的两倍。这些化合物对结核分枝杆菌及其临床分离株也表现出中等的抗结核活性，MIC 值在 8-128 μg/ml 之间。
