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

Jamie M. Singer; Bridget M. Barr; Linda L. Coughenour; Tracy F. Gregory; Michael A. Walters

doi:10.1016/j.bmcl.2005.06.097

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

Jamie M. Singer
, Bridget M. Barr
, Linda L. Coughenour
, Tracy F. Gregory
, Michael A. Walters

Research output: Contribution to journal › Article › peer-review

37 Scopus citations

Abstract

Several new, potent dopamine subtype 2 (DA D₂) 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.

Original language	English
Pages (from-to)	4560-4563
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2005.06.097
State	Published - Oct 15 2005
Externally published	Yes

Keywords

Atypical Antipsychotics
Dopamine
Serotonin

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10.1016/j.bmcl.2005.06.097

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

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 of schizophrenia.",

keywords = "Atypical Antipsychotics, Dopamine, Serotonin",

author = "Singer, \{Jamie M.\} and Barr, \{Bridget M.\} and Coughenour, \{Linda L.\} and Gregory, \{Tracy F.\} and Walters, \{Michael A.\}",

year = "2005",

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doi = "10.1016/j.bmcl.2005.06.097",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - 8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity

AU - Singer, Jamie M.

AU - Barr, Bridget M.

AU - Coughenour, Linda L.

AU - Gregory, Tracy F.

AU - Walters, Michael A.

PY - 2005/10/15

Y1 - 2005/10/15

N2 - 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.

AB - 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.

KW - Atypical Antipsychotics

KW - Dopamine

KW - Serotonin

UR - https://www.scopus.com/pages/publications/24344506610

U2 - 10.1016/j.bmcl.2005.06.097

DO - 10.1016/j.bmcl.2005.06.097

M3 - Article

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SN - 0960-894X

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EP - 4563

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

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

Abstract

Keywords

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