Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
J Med Chem, 1978/11;21(11):1116-20.
Sato M, Arimoto M, Ueno K, Kojima H, Yamasaki T, Sakurai T, Kasahara A
PMID: 31476
Impact factor: 8.039
Abstract
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.
MeSH terms
Animals; Antipsychotic Agents; Apomorphine; Butanones; Catalepsy; Humans; Lethal Dose 50; Male; Methamphetamine; Mice; Motor Activity; Rats; Stereotyped Behavior; Structure-Activity Relationship
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