含噻唑烷二酮-3-乙酸结构查尔酮衍生物的合成及抗菌活性的研究有机化学.pdfVIP

DOI: 10.6023/cjoc1107182 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 含噻唑烷二酮-3- 乙酸结构查尔酮衍生物的合成及抗菌活性的研究 孟凡领 郑昌吉 李因晶 孙良鹏 刘学坤 * 张天一 朴虎日 (延边大学药学院 长白山生物资源与功能分子教育部重点实验室 延吉 133002) 摘要 合成了一系列含噻唑烷二酮-3-乙酸结构的新型查尔酮衍生物, 并对化合物进行了抗菌活性测定. 结果显示, 一 些化合物对 4 种多重耐药菌显示出较强的抗菌活性, 其中化合物 8g, 8i, 8l 和 8m 在抗耐甲氧西林金黄色葡萄球菌的最 小抑制浓度(MIC)达到 4 µg/mL, 与对照药诺氟沙星(norfloxacin)相当. 另外, 在 64 µg/mL 浓度下, 所有化合物对大肠杆 菌 1356 均无明显抑制活性. 关键词 查尔酮; 噻唑烷二酮-3-乙酸; 抗菌活性 Synthesis and Anti-bacterial Activity of Novel Chalcone Derivatives Containing 2,4-Thiazolidinedione-3-acetic Acid Moiety Meng, Fanling Zheng, Changji Li, Yinjing Sun, Liangpeng Liu, Xuekun Zhang, Tianyi Piao, Huri* (Key Laboratory of Natural Resources of Changbai Mountain Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002) Abstract A series of novel chalcone derivatives bearing the 2,4-thiazolidinedione-3-acetic acid moieties (8a～8p) were synthesized, and evaluated for their anti-bacterial activity. The results demonstrated that some compounds presented good antimicrobial activities against four multidrug-resistant clinical isolates, among which compounds 8g, 8i, 8l and 8m with minimum inhibitory concentration (MIC) value of 4 μg/mL showed as active as the standard drug, norfloxacin, against methi- cillin-resistant S. aureu