Substituted (.omega.-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants

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Abstract
A series of substituted (.omega.-aminoalkoxy)stilbene derivatives was synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities was systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1-piperazinyl)butoxy]stilbene (20) and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives, as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. One compound exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacological tests in rats, and its therapeutic index was superior to those of the antiepileptic drugs.