Bioorganic and Medicinal Chemistry Letters p. 4560 - 4563 (2005)
Update date:2022-08-03
Topics: Medicinal chemistry Organic synthesis High-Throughput Screening In Vivo Studies In Vitro Assays Pharmacokinetics Animal Models
Singer, Jamie M.
Barr, Bridget M.
Coughenour, Linda L.
Gregory, Tracy F.
Walters, Michael A.
Several new, potent dopamine subtype 2 (DA D2) active compounds with serotonin subtype 2A (5-HT2A) 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.
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