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.
D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001362:Avoidance Learning / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003024:Clozapine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D003342:Corpus Striatum / Q000201:enzymology; D003913:Dextroamphetamine / Q000037:antagonists & inhibitors / Q000633:toxicity; D003984:Dibenzazepines / Q000138:chemical synthesis*; D004298:Dopamine / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D051381:Rats
D000067956:Adenylyl Cyclase Inhibitors; D014150:Antipsychotic Agents; D003984:Dibenzazepines; D003024:Clozapine; D003913:Dextroamphetamine; D004298:Dopamine