Several substituted pyrazolines were synthesized and characterized, and all of these pyrazolines inhibited rat brain monoamine oxidase. Evaluation of these compounds revealed appreciable anticonvulsant activity, reflected by their ability to afford protection against pentylenetetrazol-induced seizures in mice. The anticonvulsant activity possessed by these pyrazolines was unrelated to their monoamine oxidase inhibitory effectiveness.
Keyphrases 0 Pyrazolines, 1,3,5-trisubstituted-synthesis, relationship between anticonvulsant and monoamine oxidase inhibitory properties Monoamine oxidase inhibitors-substituted pyrazolines, synthesis, anticonvulsant activity Anticonvulsant activity-substituted pyrazolines, relationship to monoamine oxidase inhibitory properties Structure-activity relationshipsmonoamine oxidase inhibitory property-anticonvulsant activity
The ability of pyrazole derivatives to exhibit tranquilizing, muscle relaxant, psychoanaleptic ( l ) , hypnotic (2), and anticonvulsant (3, 4) activities prompted the synthesis of some 1,3,5-trisubstituted pyrazolines. The anticonvulsant activity of these pyrazolines was investigated against pentylenetetrazolinduced seizure in albino mice. The monoamine oxidase [EC 1.4.3.4-monoamine: 0 2 oxidoreductase (deaminating)] inhibitory property possessed by these pyrazolines was also investigated to study the biochemical mechanism of action for the anticonvulsant activity of pyrazolines. The various pyrazolines were synthesized following the methods outlined in Scheme I.