高等学校化学学报

高等学校化学学报 ›› 2006, Vol. 27 ›› Issue (2): 258.

• 研究论文 • 上一篇    下一篇

一类新型多取代嘌呤类化合物的合成及生物活性

袁德凯,李正名,赵卫光,范志金,王素华   

  1. 南开大学元素有机化学研究所, 元素有机国家重点实验室, 天津 300071
  • 收稿日期:2004-12-20 出版日期:2006-02-10 发布日期:2006-02-10
  • 通讯作者: 李正名(1931年出生), 男， 教授， 博士生导师， 中国工程院院士, 主要从事有机化学及农药化学研究. E-mail: zml@nankai.edu.cn
  • 基金资助:

     国家“八六三”计划项目(批准号： 2001AA235011)、 天津大学/南开大学联合研究院资助课题及天津市自然科学基金重点资助项目.

Synthesis and Biological Activity of a Series of Poly-substituted Purines

 YUAN De-Kai, LI Zheng-Ming, DIAO Wei-Guang, FAN Zhi-Jin, WANG Su-Hua   

  1. The Institute of Elemento\|Organic Chemistry, State Key Laboratry of Elemento-Organic
    Chemistry, Nankai University, Tianjin 300071, China
  • Received:2004-12-20 Online:2006-02-10 Published:2006-02-10
  • Contact: LI Zheng-Ming,zml@nankai.edu.cn

PDF (PC)

被引次数

11

摘要：

以4-氯-5硝基嘧啶(3)为起始物, 经胺解、还原和环合等反应, 构建了新型的多取代嘌呤-8-硫酮(6)结构. 通过化合物6与卤代物的反应, 获得了该杂环的8位巯基衍生物7a-1~7, 7b-1~5和8, 其结构经元素分析, 1H NMR, IR及MS确证. 生物活性测试结果表明,  化合物6和7具有一定的除草和抗烟草花叶病毒活性.

关键词: 多取代嘌呤-8-硫酮; 4-氯-5-硝基嘧啶; 合成; 生物活性

Abstract:

urine plays very important roles in life process, such as metabolism and heredity, while purine nucleosides and nucleotides are the key components of some important co\|enzymes nucleic acids.  Lots of compounds containing purine ring have been developed into drugs in treating cancer, virus infection and vascular disease.  In recent years, nucleic acid chemistry is also developed into a focused field.  And  derivation and selective modification of purine ring have attracted great attention of researchers.  Although N\|benzyl adenine was found to possess a good plant growth regulation (PGR) activity and used in agriculture for a long time, there is much less attention paid on purine ring than other heterocycles in agro\|chemistry field.  In order to study the synthesis and biological activities of multi-substituted purines, new poly\|substituted purine-8-thiones (6) were obtained from 4\|chloro\|5\|nitropyrimidine (3) via  a series of reactions as amination, reduction and cyclization.  After alkylation of compounds 6, 7 and 8 were obtained in high yields.  The preliminary  bioassay indicates that some of compounds  6, 7 and 8 possess moderate herbicidal and anti-TMV activities.

Key words: Poly\, substituted purine-8-thione; 4\, Chloro-5-nitropyrimidines; Synthesis; Biological activity

中图分类号: 

TrendMD: