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

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Abstract
The synthesis of 10-piperazinyl-4H-thieno[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines is described. The activity of the compounds was assessed based on their ability to produce hypothermia in mice and block a conditioned avoidance response (CAR) and produce catalepsy in rats. The results are compared with various classical and nonclassical neuroleptic drugs. A number of compounds demonstrate potency greater than clozapine and show low degree of catalepsy. This profile of activity, unlike standard neuroleptics, is presumably associated with the relative lack of extrapyramidal side effects in the clinic. The corresponding 9-piperazinyl-4H-thieno[1,4]benzodiazepines, limited analogs prepared in the respective series, were inactive.