有机化学 ›› 2008, Vol. 28 ›› Issue (03): 525-530. 上一篇    下一篇

研究简报

4-硫醚基喹唑啉类化合物的合成及抑菌活性研究

刘刚*,刘春萍,纪春暖,孙琳,温全武   

  1. (鲁东大学化学与材料科学学院 烟台 264025)
  • 收稿日期:2007-06-06 修回日期:2007-09-21 发布日期:2008-03-18
  • 通讯作者: 刘刚

Synthesis and Antifungal Activity of 4-Thioquinazoline Compounds

LIU Gang*,LIU Chun-Ping,JI Chun-Nuan,SUN Lin,WEN Quan-Wu   

  1. (School of Chemistry and Materials Science, Ludong University, Yantai 264025)
  • Received:2007-06-06 Revised:2007-09-21 Published:2008-03-18
  • Contact: LIU Gang

以4-氯喹唑啉和巯基化合物为原料, 丙酮作溶剂, 碳酸钾作缚酸剂, 合成了7个新型4-硫醚基喹唑啉类化合物. 采用1H NMR, 13C NMR, IR及元素分析对目标化合物的结构进行了表征. 生物活性测试表明, 化合物1d在50 μg•mL-1 药剂浓度下对小麦赤霉病菌、辣椒枯萎病菌、苹果腐烂病菌的抑菌活性分别达到69.5%, 71.9%和70.8%, EC50分别为25.88, 17.08和28.77 μg•mL-1.

关键词: 喹唑啉, 抑菌活性, 合成

Seven novel 4-thioquinazoline compounds were synthesized by the reaction of 4-chloroquinazoline with mercapto compounds in acetone using anhydrous K2CO3. The structures of the title compounds were characterized by elemental analyses, IR, 1H NMR and 13C NMR spectra. The results of bioassay showed that compound 1d had good antifungal activity against Fusarium graminearum, Fusarium oxysporum and Cytospora mandshurica with respective inhibition rate of 69.5%, 71.9% and 70.8% at the concentration of 50 μg•mL-1, and EC50 of 1d was 25.88, 17.08 and 28.77 μg•mL-1.

Key words: antifungal activity, quinazoline, synthesis