Synthesis and Anticonvulsant Activity of Ethyl 2,2-dimethyl-1-(2-substitutedhydrazinecarboxamido) Cyclopropanecarboxylate Derivatives

Authors

  • Min Zhong,

    1. Wuhan Economic and Technological Development Zone, School of Chemical and Environmental Engineering, Jianghan University, Wuhan, China
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  • Yongmin Zhang,

    1. Wuhan Economic and Technological Development Zone, Institute for Interdisciplinary Research, Jianghan University, Wuhan, China
    2. Institut Parisien de Chimie Moléculaire, CNRS UMR 7201, Université Pierre et Marie Curie-Paris 6, Paris, France
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  • Xianran He

    Corresponding author
    1. Wuhan Economic and Technological Development Zone, Institute for Interdisciplinary Research, Jianghan University, Wuhan, China
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Abstract

In this study on the development of new anticonvulsants, fourteen ethyl 2,2-dimethyl-1-(2-substitutedhydrazinecarboxamido) cyclopropanecarboxylate derivatives were synthesized and tested for anticonvulsant activity using the maximal electroshock, subcutaneous pentylenetetrazole screens, which are the most widely employed seizure models for early identification of candidate anticonvulsants. Their neurotoxicity was determined applying the rotorod test. Two compounds 6f and 6k showed promising anticonvulsant activities in both models employed for anticonvulsant evaluation. The most active compound 6k showed the maximal electroshock-induced seizures with ED50 value of 9.2 mg/kg and TD50 value of 387.5 mg/kg after intraperitoneally injection to mice, which provided compound 6k with a protective index (TD50/ED50) of 42.1 in the maximal electroshock test.

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