European Journal of Medicinal Chemistry 2010-09-01

N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides: synthesis and anticonvulsant activity.

Darpan Kaushik, Suroor Ahmad Khan, Gita Chawla, Suresh Kumar

文献索引：Eur. J. Med. Chem. 45 , 3943-9, (2010)

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摘要

A series of N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides were synthesized using appropriate synthetic route and characterized by elemental analysis and spectral data. The anticonvulsant activity of some of the synthesized compounds were evaluated against maximal electroshock induced seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure models in mice. The neurotoxicity were 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 compound tested, all except 5 g showed protection from seizures in both the animal models. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to phenytoin.2010 Elsevier Masson SAS. All rights reserved.