Aromatic ring functionalization of benzolactam derivatives: New potent dopamine D3 receptor ligands
Ortega R, Hübner H, Gmeiner P, Masaguer CF (2011)
Publication Language: English
Publication Type: Journal article, Original article
Publication year: 2011
Journal
Original Authors: Ortega R., Hubner H., Gmeiner P., Masaguer C.F.
Publisher: Elsevier
Book Volume: 21
Pages Range: 2670-2674
Journal Issue: 9
DOI: 10.1016/j.bmcl.2010.12.083
Abstract
Since the discovery of the dopamine D receptor, an intensive effort has been directed toward the development of potent and selective ligands in order to elucidate the function and potential therapeutic advantages of targeting D receptors. As a part of our efforts, a novel series of substituted benzolactams derivatives was synthesized mostly through palladium-catalyzed reactions. Their affinities on D -D receptors were evaluated and the data led us to highly potent D ligands, some of them highly selective for D receptor, compared to the related dopamine receptor subtypes. Functional D activity assays of the most relevant compounds have been carried out revealing antagonist as well as partial agonist activity. © 2010 Elsevier Ltd. All rights reserved.
Authors with CRIS profile
Harald Hübner
Lehrstuhl für Pharmazeutische Chemie
Peter Gmeiner
Lehrstuhl für Pharmazeutische Chemie
Additional Organisation(s)
Involved external institutions
Spain (ES)How to cite
APA:
Ortega, R., Hübner, H., Gmeiner, P., & Masaguer, C.F. (2011). Aromatic ring functionalization of benzolactam derivatives: New potent dopamine D3 receptor ligands. Bioorganic & Medicinal Chemistry Letters, 21(9), 2670-2674. https://doi.org/10.1016/j.bmcl.2010.12.083
MLA:
Ortega, Raquel, et al. "Aromatic ring functionalization of benzolactam derivatives: New potent dopamine D3 receptor ligands." Bioorganic & Medicinal Chemistry Letters 21.9 (2011): 2670-2674.
BibTeX: Download