Abstract

A series of newer derivatives 10a–n containing a 2,4-thiazolidinedione and 2-aryl-4-thiazolidinone moieties of pharmacological significance have been synthesized. The compounds were screened for their in vitro antimicrobial activity against three Gram-positive bacteria Staphylococcus aureus, Bacillus cereus, and Micrococcus luteus and three Gram-negative bacteria Pseudomonas fluorescens, Escherichia coli, and Flavobacterium devorans. Among them,10c, 10d, 10i, 10j, 10k, 10l, and 10n displayed equipotent antibacterial activity against the tested strains. All synthesized compounds were also tested for their cytotoxic activity against HeLa and MCF-7 cell lines. This study shows that all compounds were non-cytotoxicin nature, and confirmed their antimicrobial specificity apart from any general cytotoxicity. All these synthesized compounds were characterized by ¹H NMR, ¹³C NMR, and HRMS spectral techniques.

摘要

已经合成了一系列较新的衍生物10a-n，其中含有具有药理意义的 2,4-噻唑烷二酮和 2-芳基-4-噻唑烷酮部分。筛选了这些化合物对三种革兰氏阳性细菌金黄色葡萄球菌、蜡状芽孢杆菌和微球菌和三种革兰氏阴性细菌荧光假单胞菌、大肠杆菌和黄杆菌的体外抗菌活性。其中，10c、10d、10i、10j、10k、10l、10n对受试菌株显示出等效的抗菌活性。还测试了所有合成的化合物对 HeLa 和 MCF-7 细胞系的细胞毒活性。该研究表明，所有化合物都具有非细胞毒性，并证实了它们除了任何一般的细胞毒性外还具有抗菌特异性。所有这些合成的化合物均通过¹ H NMR、¹³ C NMR 和 HRMS 光谱技术进行了表征。