Title:Synthesis and Evaluation of Anticonvulsant Activities of Pyrazol yl Semicarbazones. Part II
VOLUME: 13 ISSUE: 8
Author(s):Ming-Xia Song, Yi Wu and Xian-Qing Deng
Affiliation:Medical College, Jinggangshan University, No 28, xueyuan road, Ji'an, Jiangxi, 343009, China.
Keywords:Anticonvulsant, pyrazole, semicarbazone, maximal electroshock, pentylenetetrazole.
Abstract:A series of 2-((5-aryloxy-1-methyl-3-methyl-1H-pyrazol-4-yl)methylene) hydrazinecarboxamides
(6a-6l) and 2-((5-aryloxy-1-methyl-3-phenyl-1H-pyrazol-4-yl)methylene) hydrazinecarboxamides
(7a-7l) were designed and synthesized. The maximal electroshock shock (MES) and subcutaneous
pentylenetetrazole (sc-PTZ) seizure models in mice were used to evaluate the antiepileptic
effect of compounds synthesized. Further, the acute neurotoxicity profile was also studied via the rotarod
test. The results of sc-PTZ test indicate that a majority of compounds possessed anticonvulsant
activity with long duration of protection effects. Among of them, compound 6k was found to be the
most promising one, with an ED50 value of 20.4 mg/kg (in sc-PTZ model) and a PI value of 10.8, possessing
higher anti-PTZ activity and wider safety margin than valproate and ethosuximide.
