2-芳基亚氨基-3-芳基噻唑烷-4-酮的设计、合成及抗生物膜活性
Design, synthesis, and antibiofilm activity of 2-arylimino-3-aryl-thiazolidine-4-ones.
作者信息
Pan Bin, Huang Ren-Zheng, Han Shi-Qing, Qu Di, Zhu Ming-Li, Wei Ping, Ying Han-Jie
机构信息
College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2461-4. doi: 10.1016/j.bmcl.2010.03.013. Epub 2010 Mar 7.
A series of novel 2-arylimino-3-aryl-thiazolidine-4-ones was designed, synthesized and tested for in vitro antibiofilm activity against Staphylococcus epidermidis. Among them tested, some compounds with carboxylic acid groups showed good antibiofilm activity. The antibiofilm concentration of 1x was 6.25 microM. The structure-activity relationships revealed that incorporation of 2-phenylfuran moiety could greatly enhance antibiofilm activity of thiazolidine-4-one.
设计、合成了一系列新型的2-芳基亚氨基-3-芳基噻唑烷-4-酮，并测试了它们对表皮葡萄球菌的体外抗生物膜活性。在测试的化合物中，一些含有羧酸基团的化合物表现出良好的抗生物膜活性。1x的抗生物膜浓度为6.25微摩尔。构效关系表明，引入2-苯基呋喃部分可大大增强噻唑烷-4-酮的抗生物膜活性。
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