Acta Pharmaceutica, Vol. 56 No. 3, 2006.
Original scientific paper
Synthesis of N4- (2,4-dimethylphenyl) semicarbazones as 4-aminobutyrate aminotransferase inhibitors
PERUMAL YOGEESWARI
DHARMARAJAN SRIRAM
RATHINASABAPATHY THIRUMURUGAN
LOGANTHA RAMAMOORTHY JEEWANLAL SUNIL JIT JIT
JEGADEESAN VAIGUNDA RAGAVENDRAN
RAMKUMAR KAVYA
KAVYA RAKHRA
VIVEK SARASWAT
Abstract
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 (MES), subcutaneous pentylenetetrazole (scPTZ) and subcutaneous strychnine (scSTY) 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 -aminobutyric acid levels and in vitro -aminobutyrate transaminase (Pseudomonas fluorescens) activity. Preliminary studies suggest these compounds to exhibit anticonvulsant activity via GABA-mediated mechanism.
Keywords
2,4-dimethylphenyl semicarbazones; anticonvulsants; GABA; GABA-transaminase; maximal electroshock; pentylenetetrazole; strychinine
Hrčak ID:
4539
URI
Publication date:
1.9.2006.
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