SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling.
Structure-activity relationships of a series of bis-arylic compounds, investigated as 5-HT(7)R ligands, are reported. The main structural modifications involved a central aryl moiety (phenyl, pyridine, diazine, triazine) and the nature and position of an amine-containing aliphatic chain. The affinity of the synthesized compounds (26 nM-10 microM) was systematically correlated with other previously reported series of bis-arylic ligands and rationalized by a ligand-based pharmacophore approach.
Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 6005, BP 6759, rue de Chartres, 45067 Orléans cedex 2, France.
Eduard
E
Badarau
Ryszard
R
Bugno
Franck
F
Suzenet
Andrzej J
AJ
Bojarski
Adriana-Luminita
AL
Finaru
Gérald
G
Guillaumet
D001555:Benzene Derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D011985:Receptors, Serotonin / Q000378:metabolism*; D013329:Structure-Activity Relationship
D001555:Benzene Derivatives; D008024:Ligands; D011985:Receptors, Serotonin; C104425:serotonin 7 receptor