Résumé
Mannich bases and styryl derivatives of imidazolones were evaluated for their antiparkinsonian activity. Two compounds showed potent antiparkinsonian activity. These active compounds also showed binding with dopamine receptors in striatal membrane preparation of rat brain.
Sujets)
Animaux , Antiparkinsoniens , Femelle , Imidazoles/composition chimique , Mâle , Structure moléculaire , Rats , Récepteurs dopaminergiques/métabolismeSujets)
Analgésiques , Animaux , Femelle , Mâle , Souris , Inhibiteurs de la monoamine oxydase , Quinoléines , RatsRésumé
Several 1,3,4-oxadiazol-thiones were synthesised and characterized by their melting points elemental analysis and I.R. spectra. All the oxadiazol-thiones possessed anticonvulsant activity which was reflected by protection upto 80% against pentylenetetrazole induced seizures and 40% protection against maximal electroshock induced seizures. Substantiations at position-3 of oxadiazol-thiones have shown marked effect on MAO inhibitory activity. No definite correlation between monoamine oxidase inhibitory and anticonvulsant activity could be established. It was observed that by the substitution of one, two and three methyl groups in the phenyl ring of 2-arylamino methyl side chain anticonvulsant activity against both maximal electroshock induced convulsions and pentylenetetrazol induced convulsions decreases i.e. the order of activity was found to be unsubstituted greater than monomethyl greater than dimethyl greater than trimethyl.