Studies on the anticonvulsant activity and influence on GABA-ergic neurotransmission of 1,2,4-triazole-3-thione- based compounds

Molecules. 2014 Jul 31;19(8):11279-99. doi: 10.3390/molecules190811279.

Abstract

The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one of the phenyl rings attached to 1,2,4-triazole nucleus had a substituent at the para position. The obtained results, moreover, permit us to conclude that despite the structural similarity of loreclezole (second-generation anticonvulsant drug) and the titled compounds, their anticonvulsant activity is achieved via completely different molecular mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / pharmacology*
  • Disease Models, Animal
  • GABA Agents / chemical synthesis
  • GABA Agents / pharmacology*
  • Male
  • Mice
  • Seizures / drug therapy
  • Synaptic Transmission / drug effects*
  • Toxicity Tests
  • Triazoles / chemical synthesis
  • Triazoles / pharmacology*

Substances

  • Anticonvulsants
  • GABA Agents
  • Triazoles