New sulfonamide-tethered coumarin derivatives as potential DNA gyrase inhibitors: Design, synthesis, antimicrobial evaluation, and in silico study
作者:Heba M. Abo-Salem、Eman AboBakr Ali、Shaima A. El-Mowafi、Mohamed S. Abdel-Aziz、Eslam R. El-Sawy、Hayam A. Abd El Salam
DOI:10.1016/j.molstruc.2023.136860
日期:2024.1
A new series of coumarin-6-sulfonamide derivatives 3-16 have been synthesized via simple and convenient coupling reaction of coumarin-6-sulfonyl chloride with different sulfa drugs and various amino-heterocycles. The antimicrobial activity of the new compounds was evaluated against S. aureus ATCC 6538, E. coli ATCC 25933, C. albicans ATCC 10231, and A. niger NRRL A-326. Compound 12 showed potent antimicrobial
通过香豆素-6-磺酰氯与不同磺胺类药物及多种氨基杂环的简单、便捷的偶联反应,合成了一系列新的香豆素-6-磺酰胺衍生物3-16 。评估了新化合物针对金黄色葡萄球菌ATCC 6538、大肠杆菌ATCC 25933、白色念珠菌ATCC 10231 和黑曲霉NRRL A-326 的抗菌活性。化合物 12 对所有致病菌株均表现出有效的抗菌活性,对金黄色葡萄球菌的 MIC 值为 4.88 μg/mL,对白色念珠菌的 MIC值为9.76 μg/mL ,比新霉素对照药物强 4 倍(MIC= 19.53 和 39.06 μg) /mL),对大肠杆菌的 MIC 值为 39.06 μg/mL ,与新霉素等效。同时,化合物10与新霉素对金黄色葡萄球菌和白色念珠菌具有同等功效。此外,化合物14与新霉素对抗金黄色葡萄球菌的功效相当,并且比新霉素对抗白色念珠菌的功效强2倍。进一步研究表明,化合物10和12强烈抑制DNA旋转酶(IC