Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
A series of 1-(4-fluorophenyl)-4-(1-piperidinyl)-1-butanones substituted with benzimidazole, benzotriazole, or quinoxaline at the 4 position of the piperidine ring was synthesized and subjected to neuroleptic tests. Neuroleptic activities of several compounds were comparable to those of haloperidol. In particular, 4-[4-(2,3-dihydro-2-thioxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone (10) was characterized by having a potent neuroleptic activity with less liability to the extrapyramidal side effect.
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001058:Apomorphine / Q000037:antagonists & inhibitors; D002074:Butanones / Q000138:chemical synthesis* / Q000494:pharmacology; D002375:Catalepsy / Q000139:chemically induced; D006801:Humans; D007928:Lethal Dose 50; D008297:Male; D008694:Methamphetamine / Q000037:antagonists & inhibitors; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D013239:Stereotyped Behavior / Q000187:drug effects; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D002074:Butanones; D008694:Methamphetamine; D001058:Apomorphine