Two novel series of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives were designed and synthesized, and their anti-bacterial activities evaluated. These compounds showed broad-spectrum inhibitory activities against both Gram-positive and Gram-negative bacteria with minimum inhibitory concentration (MIC) values in the range of 1–64 μg/mL. The activity of compound 6c was the more potent with MIC values of 1 μg/mL against the MRSA (3167 and 3506) strains than those of gatifloxacin, oxacillin, and norfloxacin. Compared to the previously reported rhodanine derivatives, 2-thioxothiazolidin-4-one derivatives exhibited an inhibition against Gram-negative strains due to the introduction of a 1,3,4-oxadiazole moiety, among which compounds 3 showed moderate activities against the Gram-negative bacteria (Escherichiacoli 1924) with MIC values of 16 μg/mL.

设计并合成了两种新型的3-（（5-苯基-1,3,4-恶二唑-2-基）甲基）-2-硫代噻唑啉酮-4-酮衍生物，并对其抗菌活性进行了评价。这些化合物对革兰氏阳性和革兰氏阴性细菌均具有广谱抑制活性，其最小抑菌浓度（MIC）值在1–64μg/ mL的范围内。化合物6c的抗MRSA（3167和3506）菌株的MIC值为1μg/ mL，比加替沙星，奥沙西林和诺氟沙星的活性更强。与以前报道的若丹宁衍生物相比，由于引入了1,3,4-恶二唑部分，因此2-thioxothiazolidin-4-one衍生物对革兰氏阴性菌株具有抑制作用，其中化合物3对革兰氏阴性细菌（埃希氏菌属1924年）表现出中等活性，MIC值为16μg/ mL。