Synthesis and Analysis of Anticonvulsant Activities of New 4-[2-(4- alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one Derivatives

Title:Synthesis and Analysis of Anticonvulsant Activities of New 4-[2-(4- alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one Derivatives

Volume: 12 Issue: 5

Author(s): Qing-Kun Shen, Shi-Ben Wang, Guo-Hua Gong, Xiu-Mei Yin and Zhe-Shan Quan

Affiliation:

Keywords: Anticonvulsant activity, carbamazepine, maximal electroshock test, rotarod test, synthesis, triazolone.

Abstract: The present study involved the design and synthesis of new substituted 4-[2-(4- alkoxybenzylamino) ethyl]-2H-1,2,4-triazol-3(4H)-one derivatives (8a-w) starting from 1,2- ethanediamine. The final compounds were screened for their in vivo anticonvulsant activities and neurotoxicities by maximal electroshock (MES) and rotarod tests, respectively. Among the compounds studied, 4-[2-(4-butoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one hydrochloride (8b) was found by intraperitoneal administration in mice to be the most potent compound with a median effective dose (ED50) value of 33.2 mg/kg and a high protective index (PI) value of 11.4. Compound 8b showed significant oral activity against MES-induced seizures in mice with an ED50 value of 83.1 mg/kg and a PI of 18.1. The results demonstrated that compound 8b possessed better anticonvulsant activity and higher safety than the marketed drug carbamazepine.

Cite this article as:

Shen Qing-Kun, Wang Shi-Ben, Gong Guo-Hua, Yin Xiu-Mei and Quan Zhe-Shan, Synthesis and Analysis of Anticonvulsant Activities of New 4-[2-(4- alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one Derivatives, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141111235746