title: Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.
abstract: A new group of serotoninergic 5-HT(1A) or 5-HT(7) receptor ligands was identified. These compounds were designed and synthesized on a benzimidazolone scaffold and they enrich the well-known arylpiperazine class of 5-HT ligands. Diverse pharmacomodulations induced a shift in the affinity and selectivity profile with final identification of new potent hits.
authors.affiliation: Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 6005, UFR Sciences - BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France.
authors.forename: Eduard
authors.initials: E
authors.lastname: Badarau
authors.forename: Franck
authors.initials: F
authors.lastname: Suzenet
authors.forename: Andrzej J
authors.initials: AJ
authors.lastname: Bojarski
authors.forename: Adriana-Luminiţa
authors.initials: AL
authors.lastname: Fînaru
authors.forename: Gérald
authors.initials: G
authors.lastname: Guillaumet
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry; D011485:Protein Binding; D044282:Receptor, Serotonin, 5-HT1A / Q000737:chemistry* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; C104425:serotonin 7 receptor; D044282:Receptor, Serotonin, 5-HT1A; C014353:benzimidazolone