Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation

Eduard Badarau; Franck Suzenet; Andrzej J Bojarski; Adriana-Luminiţa Fînaru; Gérald Guillaumet

doi:10.1016/j.bmcl.2009.02.008

Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1600-3. doi: 10.1016/j.bmcl.2009.02.008. Epub 2009 Feb 8.

Authors

Eduard Badarau¹, Franck Suzenet, Andrzej J Bojarski, Adriana-Luminiţa Fînaru, Gérald Guillaumet

Affiliation

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

PMID: 19237285
DOI: 10.1016/j.bmcl.2009.02.008

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.

MeSH terms

Benzimidazoles / chemistry*
Chemistry, Pharmaceutical / methods*
Drug Design
Humans
Kinetics
Ligands
Models, Chemical
Molecular Structure
Piperazines / chemistry
Protein Binding
Receptor, Serotonin, 5-HT1A / chemistry*
Receptor, Serotonin, 5-HT1A / metabolism
Receptors, Serotonin / chemistry*
Receptors, Serotonin / metabolism
Structure-Activity Relationship

Substances

Benzimidazoles
Ligands
Piperazines
Receptors, Serotonin
serotonin 7 receptor
Receptor, Serotonin, 5-HT1A
benzimidazolone