Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives

doi:10.1007/s40242-014-3173-4

高等学校化学研究 ›› 2014, Vol. 30 ›› Issue (1): 98-102.doi: 10.1007/s40242-014-3173-4

Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives

CHEN Youwei, WANG Baolei, GUO Yanjun, ZHOU Yunyun, PAN Li, XIONG Lixia, YU Shujing, LI Zhengming

State Key Laboratory of Elemento-organic Chemistry, Research Institute of Elemento-organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering(Tianjin), Nankai University, Tianjin 300071, P. R. China

收稿日期:2013-04-15 修回日期:2013-05-15 出版日期:2014-02-01 发布日期:2013-11-05
通讯作者: WANG Baolei,E-mail:nkzml@vip.163.com; LI Zhengming,E-mail:wangbaolei@126.com E-mail:nkzml@vip.163.com; wangbaolei@126.com
基金资助:
Supported by the National Basic Research Program of China(No.2010CB126106), the National Natural Science Foundation of China(Nos.21272129, 21372133), the National Key Technologies Research and Development Program, China(No. 2011BAE06B05-3) and Specialized Research Fund for the Doctorial Program of Higher Education, China(No.20110031110017).

Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives

CHEN Youwei, WANG Baolei, GUO Yanjun, ZHOU Yunyun, PAN Li, XIONG Lixia, YU Shujing, LI Zhengming

State Key Laboratory of Elemento-organic Chemistry, Research Institute of Elemento-organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering(Tianjin), Nankai University, Tianjin 300071, P. R. China

Received:2013-04-15 Revised:2013-05-15 Online:2014-02-01 Published:2013-11-05
Contact: WANG Baolei,E-mail:nkzml@vip.163.com; LI Zhengming,E-mail:wangbaolei@126.com E-mail:nkzml@vip.163.com; wangbaolei@126.com
Supported by:
Supported by the National Basic Research Program of China(No.2010CB126106), the National Natural Science Foundation of China(Nos.21272129, 21372133), the National Key Technologies Research and Development Program, China(No. 2011BAE06B05-3) and Specialized Research Fund for the Doctorial Program of Higher Education, China(No.20110031110017).

摘要/Abstract

摘要：

Caffeine is one of methyl xanthine compounds, which has the similar mode of action as ryanodine receptor insecticide. In order to find novel and efficient insecticide, structural modification of certain methyl xanthine compounds was made by introducing some common pesticidal active moieties into the structure of caffeine. Eleven novel methyl xanthine compounds were synthesized and characterized by ¹H nuclear magnetic resonance(¹H NMR), elemental analylsis or high-resolution mass spectrometry(HRMS). According to the biological activity results, it was found that these new compounds show moderate activity towards Mythimna separata Walker and Culex pipiens pallens. For example, compound 2d shows a lethality rate of 40% at 200 mg/L towards Mythimna separata Walker, compounds 2i and 2f show 56.7% and 53.3% lethality rates at 2 mg/L towards Culex pipiens pallens, which are all better than caffeine. In addition, some compounds of them show moderate antifungal activity to some plant pathogenous fungi.

关键词: Caffeine, Xanthine, Insecticidal activity, Antifungal activity

Abstract:

Key words: Caffeine, Xanthine, Insecticidal activity, Antifungal activity

CHEN Youwei, WANG Baolei, GUO Yanjun, ZHOU Yunyun, PAN Li, XIONG Lixia, YU Shujing, LI Zhengming. Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives[J]. 高等学校化学研究, 2014, 30(1): 98-102.

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Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives

Synthesis and Biological Activities of Novel Methyl Xanthine Derivatives

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