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

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

文献索引：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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被引用次数: 28

摘要

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 ...