Novas molÃculas imidazolidÃnicas: preparaÃÃo, determinaÃÃo estrutural e avaliaÃÃo da atividade anticonvulsivante

AUTOR(ES)

Manuela dos Santos Carvalho

DATA DE PUBLICAÇÃO

2005

RESUMO

Epilepsy, one of the most frequent neurological afflictions in the man, is characterized by recurrent spontaneous seizures by excessive temporary neuronal discharges resulting in uncontrolled convulsion, requires special medical attention. Until moment, the epilepsy remains subtreated the spite of the advances in the development of drugs effective for the treatment, and many patients still receive inadequate or unsatisfatory therapy. The hydantoins, a classroom of imidas cyclical, have been demonstrated as possessing good anticonvulsants properties, depending on the nature of the substitution in the hydantoin ring. The hydantoin substituted with alkyl, halogeno, trifluoromethyl, and alkoxyl groups at the phenyl ring had been found showing good anticonvulsant activity. The compounds were synthetized with imidazolidin-2,4-dione as composed of departure, followed for the reaction of N-alquilation at the N-3 position of the imidazolidine ring. The benzylphenylmethylenehydantoins were synthetized by the condensation base-catalyzed of imidazolidin-2,4-dione N-alkyleted with benzaldeydes substituted. The anticonvulsants tests had followed the method of induction for chemicalconvulsant injected way I.P. of 3,28 mg/kg of strichynin sulphate penta hydrated. The protective effect of tested compounds of the MS-6 and MS-2 injected in the dose of 100mg/kg i.p. previously 1h to the induction was observed and compared with the group it has controlled (fenitoÃna 100 mg/kg). The protective effect before the first seizure and death of the animals had been evaluated. [3-(4-methyl-benzylidene)-5-(4-methyl-benzyl)-Imidazolidin-2,4-dione] (MS-6) and [3-(4-methyl-benzylidene)-5-(4-chlorine-benzyl)-Imidazolidin-2,4-dione] (MS-2) were synthetized with satisfactory incomes and its structures had been confirmed by the methods of structural characterization of IV, RMN1H and MS. The anticonvulsant activity of the MS-2 and MS-6 was evaluated by the protection before the first seizure

ASSUNTO(S)

determinaÃÃo estrutural atividade anticonvulsivante quimica dos produtos naturais molÃculas imidazolidÃnicas

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