Synthesis, Antimicrobial Activity and Structure-Activity Relationship of Some 5-Arylidene-thiazolidine-2,4-dione Derivatives

Derivatives of the thiazolidine-2,4-dione core represent a heterocyclic class with several correlated properties. In this context, the synthesis of structural analogues of these bioactive substances becomes attractive in the field of medicinal chemistry. These analogues act as antimicrobial agents against Gram-positives pathogens. The present work aimed to synthesize 10 different derivatives of 5-arylidene-thiazolidine-2,4-dione, employing urea as the catalyst in a solvent-free reaction medium, with yields that ranged from 45 to 99%. The compounds obtained were submitted to an antimicrobial assay against S. aureus ATCC 29213. Two compounds presented minimum inhibitory concentration of 62.5 and 32.5 µg mL-1 and minimum bactericidal concentration噻唑烷-2,4-二酮（thiazolidine-2,4-dione）母核衍生物属于一类具有多种相关特性的杂环化合物。在此背景下，此类生物活性物质的结构类似物的合成在药物化学领域受到广泛关注。此类类似物可作为抗革兰氏阳性（Gram-positive）病原体的抗菌剂。本研究以合成10种不同的5-亚芳基噻唑烷-2,4-二酮（5-arylidene-thiazolidine-2,4-dione）衍生物为目标，采用尿素作为催化剂，在无溶剂反应体系中进行合成，反应产率介于45%至99%之间。将所得到的化合物针对金黄色葡萄球菌（Staphylococcus aureus）ATCC 29213开展抗菌活性测试。其中两种化合物的最低抑菌浓度分别为62.5 µg·mL⁻¹与32.5 µg·mL⁻¹，最低杀菌浓度