Lowe J A, Seeger T F, Nagel A A, Howard H R, Seymour P A, Heym J H, Ewing F E, Newman M E, Schmidt A W, Furman J S
Central Research Division, Pfizer, Inc., Groton, Connecticut 06340.
J Med Chem. 1991 Jun;34(6):1860-6. doi: 10.1021/jm00110a016.
The design and synthesis of a series of potential atypical antipsychotic agents based on the structure of 1-naphthylpiperazine are described. The incorporation of dopamine antagonist activity into the parent structure was achieved with heterocyclic surrogates for the catechol moiety of dopamine. Compound 4b from this series showed a biochemical profile that translated to behavioral activity in the rat predictive of an antipsychotic agent with a low propensity to cause extrapyramidal side effects in man.