有机化学 ›› 2012, Vol. 32 ›› Issue (01): 183-188.DOI: 10.6023/cjoc1107182 上一篇    下一篇

研究简报

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   

  1. 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
  • 收稿日期:2011-07-18 修回日期:2011-09-14 发布日期:2011-09-14
  • 通讯作者: 朴虎日 E-mail:piaohr@ybu.edu.cn
  • 基金资助:

    国家自然科学基金(No. 20962021)资助项目.

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   

  1. Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002
  • Received:2011-07-18 Revised:2011-09-14 Published:2011-09-14
  • Contact: Hu-Ri Piao E-mail:piaohr@ybu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 20962021).

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, 8l8m 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

A series of novel chalcone derivatives bearing the 2,4-thiazolidinedione-3-acetic acid moieties (8a8p) 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 methicillin- resistant S. aureus. None of the compounds exhibited obvious activity against the Gram-negative bacteria E. coli 1356 at 64 μg/mL.

Key words: chalcone, 2,4-thiazolidinedione-3-acetic acid, anti-bacterial activity