Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.

2-Amino-4-aryl-3H-1,5-benzodiazepines were prepared and evaluated for potential neuroleptic activity. Compound 60 showed some activity in the four assays; however, the activity was not consistently observed among other members of the series. The data reflected that the structural modifications led to a decrease in activity relative to clozapine. It was apparent that the 1,5-benzodiazepine portion of clozapine is not responsible for its antipsychotic activity.