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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
引用本文:孟凡领,郑昌吉,李因晶,孙良鹏,刘学坤,张天一,朴虎日.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[J].有机化学,2012,32(1):183-188.
作者姓名:孟凡领  郑昌吉  李因晶  孙良鹏  刘学坤  张天一  朴虎日
作者单位: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4μg/mL,与对照药诺氟沙星(norfloxacin)相当.另外,在64μg/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.Synthesis and Anti-bacterial Activity of Novel Chalcone Derivatives Containing 2,4-Thiazolidinedione-3-acetic Acid Moiety[J].Chinese Journal of Organic Chemistry,2012,32(1):183-188.
Authors:Meng  Fanling  Zheng  Changji  Li  Yinjing  Sun  Liangpeng  Liu  Xuekun  Zhang  Tianyi  Piao  Huri
Institution: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.aureus.None of the compounds exhibited obvious activity against the Gram-negative bacteria E.coli 1356 at 64 μg/mL.
Keywords:chalcone  2  4-thiazolidinedione-3-acetic acid  anti-bacterial activity
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