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Synthesis and biological activities of novel methyl xanthine derivatives

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Chemical Research in Chinese Universities Aims and scope

Abstract

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.

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Authors and Affiliations

  1. 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

    Youwei Chen, Baolei Wang, Yanjun Guo, Yunyun Zhou, Li Pan, Lixia Xiong, Shujing Yu & Zhengming Li

Authors
  1. Youwei Chen
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  2. Baolei Wang
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  3. Yanjun Guo
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  4. Yunyun Zhou
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  5. Li Pan
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  6. Lixia Xiong
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  7. Shujing Yu
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  8. Zhengming Li
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Corresponding author

Correspondence to Baolei Wang.

Additional information

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).

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Chen, Y., Wang, B., Guo, Y. et al. Synthesis and biological activities of novel methyl xanthine derivatives. Chem. Res. Chin. Univ. 30, 98–102 (2014). https://doi.org/10.1007/s40242-014-3173-4

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  • DOI: https://doi.org/10.1007/s40242-014-3173-4

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