有机化学 ›› 2018, Vol. 38 ›› Issue (10): 2784-2790.DOI: 10.6023/cjoc201801040 上一篇    下一篇

研究简报

含苯并噻唑的硫脲嘧啶衍生物的合成及抗菌活性评价

崔朋雷a,b, 刘娜a, 陈华a, 李小六a   

  1. a 河北大学化学与环境科学学院 河北省化学生物学重点实验室 保定 071002;
    b 河北农业大学理学院 保定 071001
  • 收稿日期:2018-01-27 修回日期:2018-03-19 发布日期:2018-06-01
  • 通讯作者: 陈华,E-mail:hua-todd@163.com E-mail:hua-todd@163.com
  • 基金资助:

    河北农业大学理工基金(No.LG20150503)资助项目.

Synthesis and Antibacterial Activity Evaluation of the Thiouracil Derivatives Containing Benzothiazole

Cui Pengleia,b, Liu Naa, Chen Huaa, Li Xiaoliua   

  1. a Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002;
    b College of Science, Agricultural University of Hebei, Baoding 071001
  • Received:2018-01-27 Revised:2018-03-19 Published:2018-06-01
  • Contact: 10.6023/cjoc201801040 E-mail:hua-todd@163.com
  • Supported by:

    Project supported by the Science and Technology Fund of Agricultural University of Hebei (No. LG20150503)

2-氨基苯并噻唑衍生物和对氯甲基苯甲酰氯反应合成中间体N-(苯并[d]噻唑-2-基)-4-(氯甲基)苯甲酰胺(5),进一步与4-氧代-6-苯基-2-硫代-1,2,3,4-四氢嘧啶-5-腈(6)反应,合成了一系列未见报道的含苯并噻唑的硫脲嘧啶类化合物7.通过红外光谱、质谱、核磁共振谱和元素分析等方法对化合物进行了结构表征.测试了化合物7对解淀粉芽孢杆菌、金黄色葡萄球菌、枯草芽孢杆菌的抑菌活性.24 h抑菌试验结果显示,部分化合物对供试的菌株具有较强的抑制活性.

关键词: 硫脲嘧啶, 苯并噻唑, 抗菌活性

A series of unreported thiouracil derivatives 7 containing a benzothiazole moiety were synthesized by the reaction of 4-oxo-6-phenyl-2-thioxo-1,2,3,4-tetrahydro-pyrimidine-5-carbonitrile (6) with N-(benzo[d]thiazol-2-yl)-4-(chloromethyl)-benzamide (5), which was prepared from the amidation of 2-aminobenzothiazole and 4-(chloromethyl)benzoyl chloride. The newly synthesized compounds 7 were characterized by IR, MS, NMR, and element analysis. All the compounds were evaluated for their antibacterial activities against Bacillus amyloliquefaciens, Staphylococcus aureus and Bacillus subtilis. The results of the 24-hour antibacterial test showed that some compounds had good inhibitory activities against the three tested strains.

Key words: thiouracil, benzothiazole, antibacterial activity