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评价不同双磺酰胺席夫碱化合物的细胞毒性、抗真菌和杀幼虫活性。

Evaluation of cytotoxic, antifungal, and larvicidal activities of different bis-sulfonamide Schiff base compounds.

机构信息

Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Adıyaman University, Adıyaman, Türkiye.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adıyaman University, Adıyaman, Türkiye.

出版信息

J Biochem Mol Toxicol. 2023 Aug;37(8):e23375. doi: 10.1002/jbt.23375. Epub 2023 May 2.

Abstract

Schiff bases (imines or azomethines) are versatile ligands synthesized from the condensation of amino compounds with active carbonyl groups and used for many pharmaceutical and medicinal applications. In our study, we aimed to determine the cytotoxic, antifungal and larvicidal activities of biologically potent bis-sulfonamide Schiff base derivatives that were re-synthesized by us. For this aim, 16 compounds were re-synthesized and tested for their cytotoxic, antifungal and larvicidal properties. Among this series, compounds A1B2, A1B4, A4B2, A4B3, and A4B4 were shown to have cytotoxic activity against tested cancer lung cell line (A549). The most potent antifungal activity was observed in compounds A2B1 and A2B2 against all fungi. A1B1 showed the strongest larvicidal effect at all concentrations at the 72nd h (100% mortality). These obtained results demonstrate that these type of bis-substituted compounds might be used as biologically potent pharmacophores against different types of diseases.

摘要

席夫碱(亚胺或偶氮化合物)是由氨基化合物与活性羰基缩合合成的多功能配体,用于许多药物和医学应用。在我们的研究中,我们旨在确定我们重新合成的具有生物活性的双磺酰胺席夫碱衍生物的细胞毒性、抗真菌和杀幼虫活性。为此,我们重新合成了 16 种化合物,并测试了它们的细胞毒性、抗真菌和杀幼虫特性。在这一系列中,化合物 A1B2、A1B4、A4B2、A4B3 和 A4B4 对测试的肺癌细胞系(A549)表现出细胞毒性活性。化合物 A2B1 和 A2B2 对所有真菌的抗真菌活性最强。在 72 小时时,A1B1 在所有浓度下表现出最强的杀幼虫效果(100%死亡率)。这些结果表明,这类双取代化合物可能作为具有生物活性的药效团,用于治疗不同类型的疾病。

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