SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling

Eduard Badarau; Ryszard Bugno; Franck Suzenet; Andrzej J Bojarski; Adriana-Luminita Finaru; Gérald Guillaumet

doi:10.1016/j.bmc.2010.01.035

SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling

Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. doi: 10.1016/j.bmc.2010.01.035. Epub 2010 Jan 18.

Authors

Eduard Badarau¹, Ryszard Bugno, Franck Suzenet, Andrzej J Bojarski, Adriana-Luminita Finaru, Gérald Guillaumet

Affiliation

¹ Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 6005, BP 6759, rue de Chartres, 45067 Orléans cedex 2, France.

PMID: 20138771
DOI: 10.1016/j.bmc.2010.01.035

Abstract

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.

MeSH terms

Benzene Derivatives / chemical synthesis*
Benzene Derivatives / chemistry
Benzene Derivatives / pharmacology
Cell Line
Humans
Ligands*
Models, Molecular*
Receptors, Serotonin / metabolism*
Structure-Activity Relationship

Substances

Benzene Derivatives
Ligands
Receptors, Serotonin
serotonin 7 receptor