Synthesis of some novel 1,2,4-triazol-3-one derivatives bearing the salicyl moiety and their anticonvulsant activities

Arch Pharm (Weinheim). 2014 Jun;347(6):449-55. doi: 10.1002/ardp.201300427. Epub 2014 Mar 13.

Abstract

A series of new 1,2,4-triazole-3-one derivatives bearing the salicyl moiety were synthesized by using microwave irradiation, and their chemical structures were identified by IR, (1) H NMR, (13) C NMR, elemental analysis, and LC-MS. The anticonvulsant activities of the compounds 4a-c, 4e, and 5a-e were evaluated by the Anticonvulsant Screening Program of the National Institute of Health, USA. The compounds had moderate anticonvulsant activities in the maximum electroshock-induced seizure and minimal clonic seizure models in mice, without any neurotoxic effects.

Keywords: Anticonvulsant activity; Microwave irradiation; Salicyl aldehyde; Triazol-3-one.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / toxicity
  • Disease Models, Animal
  • Drug Design
  • Electroshock
  • Mice
  • Molecular Structure
  • Salicylates / chemical synthesis*
  • Salicylates / pharmacology*
  • Salicylates / toxicity
  • Seizures / etiology
  • Seizures / prevention & control*
  • Structure-Activity Relationship
  • Time Factors
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology*
  • Triazoles / toxicity

Substances

  • Anticonvulsants
  • Salicylates
  • Triazoles