8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity.
Several new, potent dopamine subtype 2 (DA D(2)) active compounds with serotonin subtype 2A (5-HT(2A)) pharmacology are presented. 8-Substituted 3,4-dihydroquinolinones, tetrahydroquinolines, and N-acyl tetrahydroquinolines were evaluated in primary assays. Subtle changes on this novel scaffold translated to large changes in potency and selectivity in vitro. These compounds show promise as novel atypical antipsychotics for the treatment of schizophrenia.
Singer
Jamie M
JM
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. jamie.singer@pfizer.com
Barr
Bridget M
BM
Coughenour
Linda L
LL
Gregory
Tracy F
TF
Walters
Michael A
MA
D014150:Antipsychotic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D015363:Quinolones / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D012559:Schizophrenia / Q000188:drug therapy
D014150:Antipsychotic Agents; D015363:Quinolones