Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands
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- dc.contributor.author López Muñoz, Lauraca
- dc.contributor.author Sanz, Ferranca
- dc.contributor.author Pastor Maeso, Manuelca
- dc.contributor.author Selent, Janaca
- dc.contributor.author Loza, María I.ca
- dc.contributor.author Brea, Joséca
- dc.contributor.author Areias, Filipeca
- dc.contributor.author Ortega, Raquelca
- dc.contributor.author Masaguer, Christian F.ca
- dc.contributor.author Raviña, Enriqueca
- dc.date.accessioned 2011-07-27T08:27:54Z
- dc.date.available 2011-07-27T08:27:54Z
- dc.date.issued 2009ca
- dc.description.abstract A series of new benzolactam derivatives was synthesized and the derivatives were evaluated for their/naffinities at the dopamine D1, D2, and D3 receptors. Some of these compounds showed high D2 and/or/nD3 affinity and selectivity over the D1 receptor. The SAR study of these compounds revealed structural/ncharacteristics that decisively influenced their D2 and D3 affinities. Structural models of the complexes/nbetween some of the most representative compounds of this series and the D2 and D3 receptors were/nobtained with the aim of rationalizing the observed experimental results. Moreover, selected compounds/nshowed moderate binding affinity on 5-HT2A which could contribute to reducing the occurrence of extrapyramidal/nside effects as potential antipsychotics.
- dc.format.mimetype application/pdfca
- dc.identifier.citation Ortega R, Raviña E, Masaguer CF, Areias F, Brea J, Loza MI et al. Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands. Bioorg Med Chem Lett. 2009;19(6):1773-8. DOI: 10.1016/j.bmcl.2009.01.067
- dc.identifier.doi http://dx.doi.org/10.1016/j.bmcl.2009.01.067
- dc.identifier.issn 0960-894X
- dc.identifier.uri http://hdl.handle.net/10230/12424
- dc.language.iso engca
- dc.publisher Elsevierca
- dc.relation.ispartof Bioorganic and Medicinal Chemistry Letters. 2009;19(6):1773-8
- dc.rights © Elsevier (http://dx.doi.org/10.1016/j.bmcl.2009.01.067)ca
- dc.rights.accessRights info:eu-repo/semantics/openAccess
- dc.subject.keyword Dopamine receptors
- dc.subject.keyword Arylpiperazines
- dc.subject.keyword Benzolactams
- dc.subject.keyword Structure-activity relationship
- dc.subject.keyword Antipsychotics
- dc.subject.other Dopamina -- Receptors
- dc.subject.other Neurolèptics
- dc.title Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligandsca
- dc.type info:eu-repo/semantics/articleca
- dc.type.version info:eu-repo/semantics/publishedVersion