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A Facile Synthesis and Antimicrobial Activity Evaluation of Sydnonyl-Substituted Thiazolidine Derivatives

机译:Sydnonyl取代的噻唑烷衍生物的简便合成及抗菌活性评价

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摘要

Some new sydnonyl-substituted thiazolidine derivatives were synthesized in high yields by the modified Knoevenagel condensation of 3-aryl-4-formylsydnones with thiazolidine-2,4-dione and 2-thioxo-thiazolidine-4-one, respectively. All the synthesized thiazolidine derivatives were screened by paper-disc method to identify their antimicrobial activities against three bacteria viz. Staphylococcus aureus, Proteus vulgaris and Escherichia coli, and two fungal cultures viz. Aspergillus niger and Penicillium citrinum. The reference drugs were Norfloxacin and Griseofulvin, respectively. The screening data indicated that the tested sydnonyl-substituted thiazolidine derivatives exhibited no obvious antibacterial activity compared with the standard drug Norfloxacin. However, thiazolidine derivatives displayed significant antifungal activities against Penicillium citrinum and Aspergillus niger. Notably, all of the tested compounds showed growth inhibitory activity 1.5-4.4 times higher than that of the standard drug Griseofulvin against the two fungi.
机译:通过3-芳基-4-甲酰基sydnones分别与噻唑烷-2,4-二酮和2-硫代-噻唑烷-4-one的修饰的Knoevenagel缩合反应,高收率合成了一些新的sydnonyl取代的thiazolidine衍生物。通过纸碟法筛选所有合成的噻唑烷衍生物,以鉴定它们对三种细菌的抗菌活性。金黄色葡萄球菌,变形杆菌和大肠埃希氏菌,以及两种真菌培养物。黑曲霉和柠檬青霉。参考药物分别为诺氟沙星和灰黄霉素。筛选数据表明,与标准药物诺氟沙星相比,所测试的丁二酰基取代的噻唑烷衍生物没有表现出明显的抗菌活性。但是,噻唑烷衍生物显示出对柠檬青霉和黑曲霉的显着抗真菌活性。值得注意的是,所有测试化合物对两种真菌的生长抑制活性均比标准药物灰黄霉素高1.5-4.4倍。

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