5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
A series of new 4-aryl-5-[omega-(4-aryl-1-piperazinyl)alkyl]-2(3H)- oxazolones was synthesized and tested for neuroleptic activity in mice and rats. Several compounds exhibited interesting neuroleptic activity with very low liability to the extrapyramidal side effects. In particular the activity of 4-(4-fluorophenyl)-5-[2-[4-(3,5-dichlorophenyl)-1- piperazinyl]ethyl]-2(3H)-oxazolone (14) was greater than that of butropipazone and fluanisone, while of the same order of that of chlorpromazine; however, the product showed a longer lasting activity and minor ability to produce catalepsy as compared with the reference drugs.
Cascio
G
G
Lusofarmaco, Research Division, Milan, Italy.
Manghisi
E
E
Fregnan
G
G
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001058:Apomorphine / Q000494:pharmacology; D001362:Avoidance Learning / Q000187:drug effects; D002375:Catalepsy / Q000503:physiopathology; D004285:Dogs; D007202:Indicators and Reagents; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D009132:Muscles / Q000187:drug effects / Q000502:physiology; D010080:Oxazoles / Q000138:chemical synthesis*; D010081:Oxazolone / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013239:Stereotyped Behavior / Q000187:drug effects; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D007202:Indicators and Reagents; D010080:Oxazoles; D010879:Piperazines; D010081:Oxazolone; D001058:Apomorphine