Design, Synthesis, and Evaluation of Anticonvulsant Activities of New Triazolopyrimidine Derivatives.

ABSTRACT: Epilepsy, a severe brain disease affecting a large population, is treated mainly by antiepileptic drugs (AEDs). However, toxicity, intolerance, and low efficiency of the available AEDs have prompted the continual attempts in the discovery of new AEDs. In this study, we discovered a skeleton of triazolopyrimidine for the development of new AEDs. The design, synthesis, in vivo anticonvulsant activity evaluation of triazolopyrimidines (3a-3i and 6a-6e), and pyrazolopyrimidines (4a-4i) are reported. We found that most triazolopyrimidines showed anticonvulsive activity in the maximal electroshock (MES) and pentetrazol (PTZ)-induced seizure models. On the contrary, pyrazolopyrimidines (4a-4i) showed weak or no protective effects. Among the tested derivatives, c

SUBMITTER: Song M 

PROVIDER: S-EPMC9260081 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature