Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones
Letters in Drug Design & Discovery,
Zi-Shi Zhu, Shi-Ben Wang, Xian-Qing Deng, Da-Chuan Liu and Zhe-Shan QuanAffiliation:
College of Pharmacy, Yanbian University, No. 977, Park road, Yanji, Jilin 133002, China.
AbstractA 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.
Anticonvulsant, GABA, Maximal electroshock test, Neurotoxicity, Synthesis, Triazolone.
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