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

Radioisotope Science and Technology Divi

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

36 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

Keywords

Atypical Antipsychotics
Dopamine
Serotonin

Access to Document

10.1016/j.bmcl.2005.06.097

Cite this

@article{8e64274e55444ffdbf437eacc623d61e,

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",

month = oct,

day = "15",

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

language = "English",

volume = "15",

pages = "4560--4563",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier",

number = "20",

}

TY - JOUR

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 - http://www.scopus.com/inward/record.url?scp=24344506610&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2005.06.097

DO - 10.1016/j.bmcl.2005.06.097

M3 - Article

C2 - 16087333

AN - SCOPUS:24344506610

SN - 0960-894X

VL - 15

SP - 4560

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

Access to Document

Other files and links

Fingerprint

Cite this