Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones
Zi-Shi Zhu, Shi-Ben Wang, Xian-Qing Deng, Da-Chuan Liu and Zhe-Shan Quan
Affiliation: College of Pharmacy, Yanbian University, No. 977, Park road, Yanji, Jilin 133002, China.
Keywords: Anticonvulsant, GABA, Maximal electroshock test, Neurotoxicity, Synthesis, Triazolone.
A series of 4-butyl-5-(4-alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones (6a-6u) was designed and synthesized.
The anticonvulsant effects and neurotoxicity of the compounds were evaluated with maximal electroshock test and rotarod
test. Among the synthetic compounds, 4-butyl-5-(4-(2-fluorinebenzyl)phenyl)-2H-1,2,4-triazole-3 (4H)-one (6k) was the
most potent with ED50 value of 27.4 mg/kg and protective index (PI = TD50/ED50) value of 12.0. Besides the anti-MES efficacy,
the potency of compound 6k against seizures induced by pentylenetetrazole (PTZ), 3-mercaptopropionic acid (3-
MP), and bicuculline (BIC) was also established, which suggested that the mechanisms of action including enhancing of
GABAergic activity might be involved in its anticonvulsant activity.
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