Synthesis and Antimicrobial Evaluation of Novel Hydrazones and 1,3,4-Oxadiazoles Incorporating Bumetanide Derivatives

I. Salem, S. Mostafa, Osama I. El-Sabbag, T. Ibrahim, Ahmed Abdulrahmanf, M. M. Bendary
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引用次数: 1

Abstract

The aim of this study is to synthesize new benzenesulfonamide derivatives that possess antibacterial activity using Bumetanide as a precursor of benzenesulfonamide. A novel series of hydrazones containing benzenesulfonamides (4a-i) and 1,3,4 oxadiazole containing benzenesulfonamides (5a-e) were prepared and their antibacterial and antifungal activities were measured using microplate broth assay against Gram-positive: Staphylococcus aureus, Gram-negative: Escherichia coli and Pseudomonas aeruginosa and Fungi: Aspergillus fumigates and Candida albicans. The results showed that some of the prepared compounds exhibit a good to excellent activity against the mentioned bacteria, however all the series showed no activity against fungi. Among the series, Compound (4i) demoed an excellent antibacterial activity better than that of the standard reference (Sulfamethoxazole) against Escherichia coli, while compounds (4c, 4e, 4g) showed good activity against all tested bacterial strains equals to Sulfamethoxazole activity. Moreover, compounds (4g, 5d) exert an antimicrobial activity equals to that of Sulfamethoxazole against Pseudomonas aeruginosa, while compounds (4a, 4b, 4c, 4f, 4g, 4h) exhibit similar activity to Sulfamethoxazole against Escherichia coli.
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含布美他胺衍生物的新型腙和1,3,4-恶二唑的合成及抗菌评价
本研究的目的是利用布美他尼作为苯磺酰胺的前体合成具有抗菌活性的苯磺酰胺衍生物。制备了一系列新的含苯磺酰胺(4a-i)和含1,3,4恶二唑(5a-e)的苯磺酰胺腙,并采用微孔板培养液法测定了它们对革兰氏阳性菌金黄色葡萄球菌、革兰氏阴性菌大肠杆菌和铜绿假单胞菌以及真菌:烟熏曲霉和白色念珠菌的抑菌活性。结果表明,部分化合物对上述细菌具有较好的活性,但对真菌均无活性。其中化合物(4i)对大肠杆菌的抑菌活性优于标准参比物(磺胺甲恶唑),化合物(4c、4e、4g)对所有被试菌株的抑菌活性与磺胺甲恶唑的抑菌活性相当。此外,化合物(4g, 5d)对铜绿假单胞菌的抑菌活性与磺胺甲恶唑相当,而化合物(4a, 4b, 4c, 4f, 4g, 4h)对大肠杆菌的抑菌活性与磺胺甲恶唑相似。
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