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作为潜在抗惊厥剂的芳基氨基脲的合成。

Synthesis of aryl semicarbazones as potential anticonvulsant agents.

作者信息

Yogeeswari P, Sriram D, Veena V, Kavya R, Rakhra K, Ragavendran J Vaigunda, Mehta S, Thirumurugan R, Stables J P

机构信息

Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.

出版信息

Biomed Pharmacother. 2005 Jan-Feb;59(1-2):51-5. doi: 10.1016/j.biopha.2004.04.013. Epub 2005 Jan 26.

Abstract

A series of 4-ethoxyphenyl semicarbazones (1-10) have been synthesized using an appropriate synthetic route and characterized by elemental analyses and spectral data. The anticonvulsant activity of all the synthesized compounds was evaluated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration. Among the compounds tested, compounds except 3, 4 and 10 showed protection from seizures in both the animal models. Compounds 6 and 8 were found to increase gamma-aminobutyric acid (GABA) levels in the medulla oblongata region of the rat brain.

摘要

通过适当的合成路线合成了一系列4-乙氧基苯基氨基脲(1-10),并通过元素分析和光谱数据进行了表征。在小鼠中,针对最大电休克诱导惊厥(MES)和皮下注射戊四氮(scPTZ)诱导惊厥模型,评估了所有合成化合物的抗惊厥活性。使用转棒试验法评估神经毒性。所有受试化合物均以30、100和300mg/kg体重的剂量给药,并在给药后0.5小时和4小时的时间间隔记录抗惊厥活性。在所测试的化合物中,除3、4和10之外的化合物在两种动物模型中均表现出对惊厥的保护作用。发现化合物6和8可提高大鼠脑延髓区域的γ-氨基丁酸(GABA)水平。

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