Liu Jia-Chun, Zheng Chang-Ji, Wang Meng-Xiao, Li Ya-Ru, Ma Long-xu, Hou Shao-Pu, Piao Hu-Ri
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University, College of Pharmacy, Yanji, Jilin Province 133002, PR China.
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University, College of Pharmacy, Yanji, Jilin Province 133002, PR China.
Eur J Med Chem. 2014 Mar 3;74:405-10. doi: 10.1016/j.ejmech.2013.12.054. Epub 2014 Jan 8.
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.
设计并合成了两个新型的3-((5-苯基-1,3,4-恶二唑-2-基)甲基)-2-硫代噻唑烷-4-酮衍生物系列，并对其抗菌活性进行了评估。这些化合物对革兰氏阳性菌和革兰氏阴性菌均表现出广谱抑制活性，最低抑菌浓度（MIC）值在1-64μg/mL范围内。化合物6c的活性更强，对耐甲氧西林金黄色葡萄球菌（MRSA，菌株3167和3506）的MIC值为1μg/mL，优于加替沙星、苯唑西林和诺氟沙星。与先前报道的罗丹宁衍生物相比，由于引入了1,3,4-恶二唑部分，2-硫代噻唑烷-4-酮衍生物对革兰氏阴性菌株表现出抑制作用，其中化合物3对革兰氏阴性菌（大肠杆菌1924）表现出中等活性，MIC值为16μg/mL。
