8-Substituted 3, 4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity

JM Singer, BM Barr, LL Coughenour, TF Gregory…

Index: Singer, Jamie M.; Barr, Bridget M.; Coughenour, Linda L.; Gregory, Tracy F.; Walters, Michael A. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4560 - 4563

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Citation Number: 28

Abstract

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 ...

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