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Synthesis and potential anticonvulsant activity of new aryl sulfonyl semicarbazide derivatives

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Abstract

In the present study on the development of new anticonvulsants, twelve new aryl sulfonyl semicarbazide derivatives were synthesized and tested for anticonvulsant activity using maximal electroshock (MES), subcutaneous pentylenetetrazole screens. Their neurotoxicity was determined by the rotorod test. The most active compound 5i showed the MES-induced seizures with ED50 value of 7.3 mg/kg and TD50 value of 402.3 mg/kg after intraperitoneally injection to mice, which provided compound 5i with a protective index (TD50/ED50) of 55.1 in the MES test.

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Acknowledgments

This work is supported by National Science Foundation of China (NSFC) (Grant No: 21302065), Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry of China and Technology Foundation for Selected Overseas Chinese Scholar, Ministry of Personnel of China.

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Authors and Affiliations

  1. Institute for Interdisciplinary Research, Jianghan University, Wuhan Economic and Technological Development Zone, Wuhan, 430056, People’s Republic of China

    Yousong Nie, Min Zhong, Zhiyuan Jiang, Jian Sun, Yangguang Gao, Fei Ding, Hang Li, Yongmin Zhang & Xianran He

  2. Key Laboratory of Optoelectronic Chemical Materials and Devices, Ministry of Education, School of Chemical and Environmental Engineering, Jianghan University, Wuhan, 430056, People’s Republic of China

    Yousong Nie, Min Zhong, Zhiyuan Jiang, Jian Sun & Xianran He

  3. Institut Parisien de Chimie Moléculaire, CNRS UMR 7201, Université Pierre et Marie Curie-Paris 6, 4 Place Jussieu, 75005, Paris, France

    Yongmin Zhang

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  1. Yousong Nie
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  2. Min Zhong
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Correspondence to Xianran He.

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Nie, Y., Zhong, M., Jiang, Z. et al. Synthesis and potential anticonvulsant activity of new aryl sulfonyl semicarbazide derivatives. Med Chem Res 25, 1425–1432 (2016). https://doi.org/10.1007/s00044-016-1582-2

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  • DOI: https://doi.org/10.1007/s00044-016-1582-2

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