Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones

Title:Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones

Volume: 11 Issue: 5

Author(s): Zi-Shi Zhu, Shi-Ben Wang, Xian-Qing Deng, Da-Chuan Liu and Zhe-Shan Quan

Affiliation:

Keywords: Anticonvulsant, GABA, Maximal electroshock test, Neurotoxicity, Synthesis, Triazolone.

Abstract: 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.

Cite this article as:

Zhu Zi-Shi, Wang Shi-Ben, Deng Xian-Qing, Liu Da-Chuan and Quan Zhe-Shan, Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones, Letters in Drug Design & Discovery 2014; 11 (5) . https://dx.doi.org/10.2174/1570180810666131122003939

DOI https://dx.doi.org/10.2174/1570180810666131122003939	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X