Acta Pharm. 56 (2006) 259-272[ Full paper in PDF ]
Several 2,4-dimethylphenyl substituted semicarbazones were synthesized in three steps involving aryl urea and aryl semicarbazide formations. The structures were confirmed by spectral and elemental analyses. All the compounds were evaluated for anticonvulsant activity by using a series of test models including maximal electroshock seizure, subcutaneous pentylenetetrazole and subcutaneous strychnine seizure threshold tests. The compounds were also evaluated for behavioural impairement and depression activity. In the neurochemical investigation, potent compounds were evaluated for their effects on rat brain gamma-aminobutyric acid (GABA) levels and in vitro gamma-aminobutyrate transaminase (Pseudomonas fluorescens) activity. Preliminary studies suggest these compounds exhibit anticonvulsant activity via a GABA-mediated mechanism.
Keywords: 2,4-dimethylphenyl semicarbazones, anticonvulsants, GABA, GABA-transaminase, maximal electroshock, pentylenetetrazole, strychinine