Synthesis and potential anticonvulsant activity of new aryl sulfonyl semicarbazide derivatives

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作者
Yousong Nie
Min Zhong
Zhiyuan Jiang
Jian Sun
Yangguang Gao
Fei Ding
Hang Li
Yongmin Zhang
Xianran He
机构
[1] Jianghan University,Institute for Interdisciplinary Research
[2] Jianghan University,Key Laboratory of Optoelectronic Chemical Materials and Devices, Ministry of Education, School of Chemical and Environmental Engineering
[3] Université Pierre et Marie Curie-Paris 6,Institut Parisien de Chimie Moléculaire, CNRS UMR 7201
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Aryl sulfonyl semicarbazide; MES; PTZ; Neurotoxicity;
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摘要
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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页码:1425 / 1432
页数:7
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