磺胺甲恶唑类药物衍生的希夫碱和1,3 -恶氮平类化合物的合成、表征和生物活性研究

E. Mousa, I. Jassim
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引用次数: 0

摘要

本研究采用经典的希夫碱法,由磺胺甲恶唑类药物与芳香族醛反应合成了一些新的希夫碱化合物[1‐6],然后用丁二酸酐处理希夫碱得到了恶氮平类化合物[7-11],并用熔点、FT‐IR、1H NMR和质谱对其进行了表征。采用琼脂扩散盘法对合成的部分化合物进行了对金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌3种病原菌及念珠菌的体外抑菌活性评价。结果表明,与母体药物的生物活性相比,部分衍生物具有较好的抗菌活性。
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SYNTHESIS, CHARACTERIZATION, AND STUDY THE BIOLOGICAL ACTIVITY OF SOME SCHIFF'S BASES, AND 1,3 - OXAZEPINE COMPOUNDS DERIVED FROM SULFAMETHOXAZOLE DRUG
This study including synthesis of some new Schiff bases compounds [1‐6] from the reaction of Sulfamethoxazole drug with some aromatic aldehydes in classical Schiff base method then treatment Schiff bases with succinic anhydride to get oxazepines rings [7-11]These derivatives were characterized by melting point, FT‐IR, 1H NMR and mass spectra. Some of synthesized compounds were evaluated in vitro for their antibacterial activities against three kinds of pathogenic strains Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa by agar diffusion disk method, and against the fungal species (Candida). The results showed that some of these derivatives have good antibacterial activities compared to biological activity of parent drug.
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