有机化学 ›› 2008, Vol. 28 ›› Issue (07): 1268-1272. 上一篇    下一篇

研究简报

6-溴-4-烃硫基喹唑啉类化合物的合成及抑菌活性研究

马 耀 ; 刘 芳; 严 凯; 宋宝安*; 杨 松 ;
胡德禹; 金林红 ; 薛 伟
  

  1. (贵州大学精细化工研究开发中心 教育部绿色农药和生物工程重点实验室 贵阳 550025)
  • 收稿日期:2007-10-07 修回日期:2008-02-25 发布日期:2008-07-28
  • 通讯作者: 宋宝安

Synthesis and Antifungal Bioactivity of 6-Bromo-4-alkylthio-quinazoline Derivatives

MA, Yao ; LIU, Fang ; YAN, Kai ; SONG, Bao-An* ; YANG, Song ;
HU, De-Yu; JIN, Lin-Hong; XUE, Wei
  

  1. (Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025)
  • Received:2007-10-07 Revised:2008-02-25 Published:2008-07-28
  • Contact: SONG, Bao-An

以6-溴-4-巯基喹唑啉和卤代烃为原料, 用相转移催化法合成了10个新的6-溴-4-烃硫基取代喹唑啉类化合物. 化合物经1H NMR, 13C NMR, IR及元素分析证明其结构. 初步生物活性试验结果表明, 在50 mg•L-1浓度下, 化合物6g对小麦赤霉病菌、辣椒枯萎菌、苹果腐烂菌抑制率分别为63.8%, 51.9%, 55.1%, 与对照药剂恶霉灵抑制活性相当.

关键词: 溴, 硫醚, 抑菌活性, 喹唑啉

Ten new 6-bromo-4-alkylthioquinazoline compounds were synthesized by the reaction of 6-bromo-4-thiolquinazoline with alkylhalide under the conditions of phase-transfer catalysis. The structures of the new compounds were characterized by 1H NMR, 13C NMR, IR spectra and elemental analyses. Bioac-tivity of the new compounds was tested. The preliminary bioassay showed that compound 6g had certain an-tifungal activities against Fusarium graminearum, Cytospora mandshurica and Fusarium oxysporum with rate of 63.8%, 51.9% and 55.1% at the concentration of 50 mg•L-1, respectively, similarly to that of control (hymexozole).

Key words: bromine, thioether, antifungal activity, quinazoline