Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.
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.
Badarau
Eduard
E
Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 6005, UFR Sciences - BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France.
Suzenet
Franck
F
Bojarski
Andrzej J
AJ
Fînaru
Adriana-Luminiţa
AL
Guillaumet
Gérald
G
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
D001562:Benzimidazoles; D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; C104425:serotonin 7 receptor; D044282:Receptor, Serotonin, 5-HT1A; C014353:benzimidazolone