Screening investigation of novel 1,2,4-triazole-3-thione derivatives on anticonvulsant activity

Abstract

1,2,4-triazole and its derivatives are present in many biologically active aromatic compounds that have different biological properties and clinical applications including anticonvulsant activity. The number of studies in this direction is increasing. Therefore, based on the results of previous computer predictions, 8 novel 1,2,4-triazole-3-thione derivatives have been synthesized in the Department of Pharmaceutical Chemistry at the National Pharmacy University of Ukraine. The screening test of novel 1,2,4-triazole-3-thione derivatives on anticonvulsant activity in PTZ-induced seizures was conducted on mice. Among test substances revealed were those, which in the dose of 100 mg/kg showed moderate anticonvulsive effect and which were non-inferior to "reference drug" sodium valproate by some parameters. Screening results have confirmed the reasonability of in-depth anticonvulsive activity study of substances-leaders, pharmacological study of their mechanism of action, spectrum of anticonvulsant activity, concurrent types of pharmacological activity, dose-dependence of effect and safety.