二茂铁基氨基噻唑类化合物的合成及其抗菌活性研究  

Synthesis and antibacterial activity of ferrocene-based aminothiazoles

作　　者：高婷妤 孙福泽 赵欣悦 文宝涵 高思旸 李阳[1] 张红[1] GAO Ting-yu;SUN Fu-ze;ZHAO Xin-yue;WEN Bao-han;GAO Si-yang;LI Yang;ZHANG Hong(College of Chemistry and Materials Engineering,Bohai University,Jinzhou 121000,China)

机构地区：[1]渤海大学化学与材料工程学院,辽宁锦州121000

出　　处：《化学研究与应用》2022年第9期2019-2028,共10页Chemical Research and Application

基　　金：辽宁省教育厅项目(LQ2019006)资助;辽宁省科技厅博士启动项目(2019-BS-004)资助;辽宁省大学生创新创业项目(S202010167040)资助。

摘　　要：利用溴乙酰基二茂铁为底物,与芳基取代硫脲在回流的乙醇介质中,以三乙胺作为碱,有效进行了Hantzsc反应,合成了一系列结构新颖的二茂铁基取代的氨基噻唑类化合物。选用四种菌株为研究对象,进行了初步的体外抗菌活性实验。结果表明,含有4-甲氧基取代的化合物7d和4-氟取代的化合物7h对革兰氏阳性菌枯草芽孢杆菌和革兰氏阴性菌大肠杆菌表现出很好的抑制活性,其MIC值分别为15.625/15.625μg/mL和15.625/7.8125μg/mL,相当或好于参考药物环丙沙星的活性。A facile and general synthesis of a series of structurally intriguing and ferrocene-based aminothiazoles had been achieved in good yields through the Hantzsch reaction of bromoacetylferrocene with various aryl thioureas in refluxing ethanol medium with the presence of Et3N as base.A preliminary screening for their in vitro antibacterial activities against four bacterial strains revealed that the compounds 7d and 7h with 4-OMe and 4-F substitution showed significant antibacterial activities against the Gram(+)bacterial B.subtilis and Gram(-)E.coli with the MIC values of 15.625/15.625μg·mLand 15.625/7.8125μg·mL,respectively,being equipotent or even better than the reference drug ciprofoxacin.

关 键 词：二茂铁 氨基噻唑 Hantzsch反应 硫脲 抗菌活性 

分 类 号：O625[理学—有机化学]