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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (08): 1252-1257. 上一篇    下一篇

研究论文

C(2)-酰胺基取代的1,5-苯并硫氮杂卓的合成及抑菌活性的研究

李文红3，张玲芬1，刘薇2，杜星琼2，李媛*,1   

  1. (1河北师范大学化学与材料科学学院 石家庄 050016)
    (2河北师范大学生命科学学院 石家庄 050016)
    (3河北工业职业技术学院环境与化学工程系 石家庄 050091)
  • 收稿日期:2010-12-30 修回日期:2011-04-22 发布日期:2011-05-03
  • 通讯作者: 李媛 E-mail:yuanli@mail.hebtu.edu.cn
  • 基金资助:

    国家自然科学基金;河北省自然科学基金

Synthesis and Antifungal Activity of 2-Carboxamide-4-aryl- 1,5-benzothiazepines

Li Wenhong3 Zhang Lingfen1 Liu Wei2 Du Xingqiong2 Li Yuan*,1   

  1. (1 College of Chemistry & Material Science, Hebei Normal University, Shijiazhuang 050016)
    (2 College of Life Sciences, Hebei Normal University, Shijiazhuang 050016)
    (3 Environment and Chemical Engineering, Hebei College of Industry and Technol-ogy, Shijiazhuang 050091)
  • Received:2010-12-30 Revised:2011-04-22 Published:2011-05-03

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设计合成了三类C(2)酰胺基取代的1,5-苯并硫氮杂衍生物: 2-酰胺基(N-芳基)-4-芳基-1,5-苯并硫氮杂、2-酰胺基(N-烷基)-4-芳基-1,5-苯并硫氮杂和2-酰胺基(N,N-二烷基)-4-芳基-1,5-苯并硫氮杂, 其结构用元素分析, IR, MS及1H NMR确证. 测定了目标化合物的抑真菌活性, 结果表明部分化合物对新生隐球菌具有中等强度的抑真菌活性. 还研究了2-酰胺基-4-芳基-1,5-苯并硫氮杂的合成反应条件.

关键词: 1,5-苯并硫氮杂, 酰胺, 抑菌活性

Three kinds of 2-carboxamide-1,5-benzothiazepines including 2-carboxamide(N-aryl)-4-aryl, 2-carboxamide-(N-alkyl)-4-aryl and 2-carboxamide-(N,N-alkyl)-4-aryl-1,5-benzothiazepines were designed and synthesized, and their structures were characterized by elemental analysis, IR, 1H NMR, and MS techniques. Their antifungal activities against some fungi were evaluated, and the results indicated that some of them showed moderate fungicidal activities in vitro against C. neoformans. The synthesis condi-tions of the title compounds were also investigated.

Key words: 1,5-benzothiazepine, carboxamide, antifungal activity