Synthesis, Characterization, and Study of Antibacterial Activity of Some New Amphiphilic Sulfamethoxazole Derivatives

H. Chfat, E. Zimam
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Abstract

nucleus was functionalized with sodium azide to produce 4-azido-N-(5-methylisoxazol-3-yl)benzenesulfonamide. The end 1,2,3-triazoles were synthesized via a click reaction of the azide compound and triple bond derivatives that attached with alkyl chain or phenyl group in good yields. The structures of all prepared compounds were identified by using NMR and IR techniques. The synthesized compounds were screened for their in vitro antibacterial activity against one gram-positive bacteria S. aureus and one gram-negative bacteria E. coli. Among the synthesized compounds, compound 12 was found to be the most potent against staphylococcus aureus with MIC = 20 μg/mL compared with the other prepared compounds. Whereas compound 15 was found to be the most potent against Escherichia coli with MIC = 21 μg/mL compared with the other end compounds.
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新型两亲性磺胺甲恶唑衍生物的合成、表征及抗菌活性研究
核被叠氮化钠功能化,得到4-叠氮- n -(5-甲基异恶唑-3-基)苯磺酰胺。通过叠氮化合物与烷基链或苯基连接的三键衍生物的连锁反应合成了末端1,2,3-三唑,收率较高。利用核磁共振和红外光谱技术对所制备化合物的结构进行了鉴定。对合成的化合物进行体外抑菌活性筛选,测定其对1种革兰氏阳性菌金黄色葡萄球菌和1种革兰氏阴性菌大肠杆菌的抑菌活性。在所合成的化合物中,化合物12对金黄色葡萄球菌的抑制作用最强,MIC = 20 μg/mL。而化合物15对大肠杆菌的抑制作用最强,其MIC值为21 μg/mL。
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