化学学报 ›› 2010, Vol. 68 ›› Issue (23): 2414-2420. 上一篇    下一篇

研究论文

吡唑三杂环化合物的制备表征及生物活性的研究

夏庆春,何其庄*,许东芳,孙大志,彭子飞   

  1. (上海师范大学生命与环境科学学院 上海 200234)
  • 投稿日期:2010-05-18 修回日期:2010-07-25 发布日期:2010-08-09
  • 通讯作者: 何其庄 E-mail:hqz@shnu.edu.cn

Synthesis, Characterization and Antibacterial of Five-Membered Heterocycles

XIA Qing-Chun, HE Qi-Zhuang, XU Dong-Fang, SUN Da-Zhi, PENG Zi-Fei   

  1. (Department of Chemistry, Shanghai Normal University, Shanghai 200234)
  • Received:2010-05-18 Revised:2010-07-25 Published:2010-08-09

以1,3-二苯基-4-吡唑甲醛为原料, 合成中间体吡唑腙和吡唑基氨基硫脲, 进一步合成出一系列新颖的含有1,3,4-噁二唑, 1,2,4-三氮唑和1,3,4-噻二唑的吡唑三杂环的化合物, 通过抑菌圈法和营养肉汤法对所制备的化合物的抗菌活性进行了测试, 测试结果表明: 3-芳基-4-(1,3-二苯基-4-吡唑甲酰基)-1,2,4-三唑啉-5-硫酮对金黄色葡萄球菌具有良好的抗菌活性.

关键词: 吡唑, 噻二唑, 噁二唑, 三氮唑, 抗菌活性

In this article, a new series of 1,3,4-oxadiazoles, 1,2,4-triazoles, and 1,3,4-thiadiazoles were synthesized from the intermediates of hydrazone and thiosemicarbazide derivatives. All the compounds were evaluated for in vitro antibacterial activity using method of paper disc diffusion and nutrition broth dilution. The antibacterial data revealed that 3-aryl-4-(1,3-diphenyl-4-pyrazole-formyl)-1,2,4-triazoline-5-thione showed good activity against tested Gram-positive bacteria.

Key words: pyrazole, thiadiazole, oxadiazole, triazolam, antibacterial activity