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Benzothiazole incorporated thiazolidin-4-ones and azetidin-2-ones derivatives: Synthesis and in vitro antimicrobial evaluation
Arabian Journal of Chemistry ( IF 5.3 ) Pub Date : 2016-11-01 , DOI: 10.1016/j.arabjc.2012.04.004
Sadaf J. Gilani , K. Nagarajan , Surya P. Dixit , M. Taleuzzaman , Suroor A. Khan

Abstract In this study, a series of novel thiazolidin-4-ones ( 5a – g ) and azetidin-2-ones ( 6a – g ) were synthesized from N -(6-chlorobenzo[ d ]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria ( Staphylococcus aureus ), three Gram (−) bacteria ( Escherichia coli , Pseudomonas aeruginosa, Klebsiella pneumoniae ) and five fungi ( Candida albicans , Aspergillus niger , Aspergillus flavus , Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5–200 μg/mL in DMSO. It has been observed that azetidin-2-ones derivatives are found to be more active than thiazolidin-4-ones derivatives against all pathogenic bacterial and fungal strains.

中文翻译:

苯并噻唑并入 thiazolidin-4-ones 和 azetidin-2-ones 衍生物:合成和体外抗菌评估

摘要 本研究以N-(6-氯苯并[d]噻唑-2-基)肼甲酰胺为原料合成了一系列新型噻唑烷-4-酮(5a-g)和氮杂环丁烷-2-酮(6a-g)。苯并噻唑类的衍生物。研究了标题化合物衍生物对一种革兰氏 (+) 细菌(金黄色葡萄球菌)、三种革兰氏 (-) 细菌(大肠杆菌、铜绿假单胞菌、肺炎克雷伯菌)和五种真菌(白色念珠菌、黑曲霉、黄曲霉)的抗菌特性。 Monascus purpureus 和 Penicillium citrinum) 使用连续平板稀释法。抗菌和抗真菌筛选数据的研究表明,所有测试化合物在 DMSO 中的浓度为 12.5-200 μg/mL 时均显示出中等至良好的抑制作用。
更新日期:2016-11-01
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