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 selectiv...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-03, Vol.19 (6), p.1600-1603
Main Authors: BADARAU, Eduard, SUZENET, Franck, BOJARSKI, Andrzej J, FINARU, Adriana-Luminita, GUILLAUMET, Gérald
Format: Article
Language:English
Subjects:
Benzimidazoles - chemistry
Biological and medical sciences
Chemistry, Pharmaceutical - methods
Drug Design
Humans
Kinetics
Ligands
Medical sciences
Models, Chemical
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperazines - chemistry
Protein Binding
Receptor, Serotonin, 5-HT1A - chemistry
Receptor, Serotonin, 5-HT1A - metabolism
Receptors, Serotonin - chemistry
Receptors, Serotonin - metabolism
Serotoninergic system
Structure-Activity Relationship
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.02.008