Heteroarenobenzodiazepines. 3. 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics

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Abstract
A series of 4-substituted 10H-thieno[2,3-b][1,5]benzodiazepines was synthesized. The compounds were assessed for their ability to block a conditioned avoidance response (CAR) and to produce catalepsy in rats and were compared with several typical and atypical neuroleptics. The compounds which inhibit CAR at doses which produce no catalepsy are believed to cause less extrapyramidal side effects in the clinic. A number of compounds show potent neuroleptic activity, yet maintain a favorable separation of activity on the 2 parameters. Three 5-piperazinyl-10H-thieno[2,3-b][1,4]benzodiazepine derivatives analogous to compounds in the [1,5] series were prepared for comparison and were inactive.