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某些法玛赞-磺胺衍生物的合成、计算机模拟生化性质及体外抗菌活性

Synthesis, In-Silico Biochemical Properties, and In-Vitro Antimicrobial Activity of Some Farmazans-Sulfonamide Derivatives.

作者信息

Almehmadi Mazen, Allahyani Mamdouh, Alsuwat Meshari A, Asif Mohammad

机构信息

Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, Taif University, P.O. Box 11099, 21944, Taif, Kingdom of Saudi Arabia.

Department of Pharmaceutical Chemistry, Era College of Pharmacy, Era University, 226003, Lucknow, Uttar Pradesh, India.

出版信息

Chem Biodivers. 2025 Mar;22(3):e202402488. doi: 10.1002/cbdv.202402488. Epub 2024 Nov 20.

Abstract

The low effectiveness of currently available antibiotics is driving efforts worldwide to generate new antimicrobial drugs. So, we synthesized some new formazan derivatives containing sulfonamide moiety, and assessed their in-silico biochemical properties as well as in-vitro antibacterial activity against some pathogenic Gram-positive (B. subtilis and S. aureus) and Gram-negative (E. coli and S. thyphi) bacteria and fungi (C. albicans and A. niger). These formazan derivatives were synthesized by condensing sulphanilamide with benzaldehyde in the presence of glacial acetic acid and ethanol produced a Schiff base of sulfonamide (1). After this compound 1 was reacted with substituted benzene diazonium chlorides (2a-g) by condensation reaction yields formazan derivatives (3a-g). The structures of synthesized compounds were characterized on the basis analytical and spectral (IR, H-NMR, and mass) data. Agar diffusion method was utilized to assess the antibacterial activity of the synthesized compounds by measuring the zone of inhibition against tested strains of bacteria and fungi. Ciprofloxacin and ketoconazole were used as reference drugs. The result exhibited that synthesized compounds have demonstrated satisfactory in-silico biochemical properties as well as significant level of antibacterial activity.

摘要

目前可用抗生素的低效性促使全球致力于研发新型抗菌药物。因此,我们合成了一些含有磺酰胺部分的新型甲臜衍生物,并评估了它们的计算机模拟生化特性以及对一些致病性革兰氏阳性菌(枯草芽孢杆菌和金黄色葡萄球菌)、革兰氏阴性菌(大肠杆菌和伤寒沙门氏菌)和真菌(白色念珠菌和黑曲霉)的体外抗菌活性。这些甲臜衍生物是通过在冰醋酸和乙醇存在下将磺胺与苯甲醛缩合生成磺胺席夫碱(1)而合成的。在此之后,化合物1与取代苯重氮氯化物(2a - g)通过缩合反应生成甲臜衍生物(3a - g)。合成化合物的结构通过分析和光谱(红外、氢核磁共振和质谱)数据进行表征。采用琼脂扩散法通过测量对受试细菌和真菌菌株的抑菌圈来评估合成化合物的抗菌活性。环丙沙星和酮康唑用作参考药物。结果表明,合成化合物具有令人满意的计算机模拟生化特性以及显著的抗菌活性水平。

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