Azetidine derivatives of tricyclic antidepressant agents

Abstract

Tricyclic derivatives of azetidine were synthesized and screened for their potential antidepressant activity [in mice]. The active series had the tricyclic rings attached to position 1 and a basic group in position 3 of the azetidine. The most interesting compounds were comparable to the reference standards for reserpine antagonism in mice, the most active being the dextrorotatory methylamino derivative 84 [(+)-1-(6,11-dihydrodibenzo[b,e]oxepinyl)-3-(methylamino)azetidine hemifumarate]. The pharmacological profile classifies it as a CNS stimulant devoid of peripheral anticholinergic activity.