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

IF 2.3 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemistry & Biodiversity Pub Date : 2024-10-24 DOI:10.1002/cbdv.202402488
Mazen Almehmadi, Mamdouh Allahyani, Meshari A Alsuwat, Mohammad Asif
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引用次数: 0

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, 1H-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.

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一些含磺酰胺分子的法马赞衍生物的合成、体内生化性质和体外抗菌活性。
现有抗生素疗效不佳,促使全世界都在努力开发新的抗菌药物。我们制造了几种新型的蚁酸化学物质,包括磺酰胺,并评估了它们对细菌的作用。因此,我们尝试将甲臢和磺酰胺的分子结合起来,生产出新的衍生物或更有效的抗菌药物。磺胺与苯甲醛在冰醋酸和乙醇存在下缩合,产生磺酰胺的希夫碱,在缩合过程中与取代的苯重氮氯化物(2a-g)结合,产生甲臢衍生物(3a-g)。根据分析和光谱数据(红外光谱、1HNMR 和质量),描述了所有合成化合物的结构,这些结构与建议的结构非常吻合。以环丙沙星和酮康唑为参照药物,采用琼脂扩散法测量合成化合物对有害细菌和真菌菌株的抑制区,以评估其抗菌活性。与常规方法不同的是,所研究的每个分子都表现出了显著的抗菌活性。
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来源期刊
Chemistry & Biodiversity
Chemistry & Biodiversity 环境科学-化学综合
CiteScore
3.40
自引率
10.30%
发文量
475
审稿时长
2.6 months
期刊介绍: Chemistry & Biodiversity serves as a high-quality publishing forum covering a wide range of biorelevant topics for a truly international audience. This journal publishes both field-specific and interdisciplinary contributions on all aspects of biologically relevant chemistry research in the form of full-length original papers, short communications, invited reviews, and commentaries. It covers all research fields straddling the border between the chemical and biological sciences, with the ultimate goal of broadening our understanding of how nature works at a molecular level. Since 2017, Chemistry & Biodiversity is published in an online-only format.
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