Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com

Hervé Geneste; Gisela Backfisch; Wilfried Braje; Jürgen Delzer; Andreas Haupt; Charles W Hutchins; Linda L King; Wilfried Lubisch; Gerd Steiner; Hans-Jürgen Teschendorf; Liliane Unger; Wolfgang Wernet

doi:10.1016/j.bmcl.2005.10.035

Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com

Bioorg Med Chem Lett. 2006 Feb;16(3):658-62. doi: 10.1016/j.bmcl.2005.10.035. Epub 2005 Nov 2.

Authors

Hervé Geneste¹, Gisela Backfisch, Wilfried Braje, Jürgen Delzer, Andreas Haupt, Charles W Hutchins, Linda L King, Wilfried Lubisch, Gerd Steiner, Hans-Jürgen Teschendorf, Liliane Unger, Wolfgang Wernet

Affiliation

¹ Abbott GmbH & Co. KG, Discovery Research, D-67008 Ludwigshafen, Germany.

PMID: 16271293
DOI: 10.1016/j.bmcl.2005.10.035

Abstract

The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.

MeSH terms

Animals
Benzazepines / chemical synthesis*
Benzazepines / pharmacology
Dopamine Antagonists / chemical synthesis*
Dopamine Antagonists / pharmacology
Models, Molecular
Molecular Structure
Quinolones / chemical synthesis*
Quinolones / pharmacology
Rats
Receptors, Dopamine D3 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzazepines
Dopamine Antagonists
Quinolones
Receptors, Dopamine D3