New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation

J Enzyme Inhib Med Chem. 2010 Jun;25(3):301-5. doi: 10.3109/14756360903179393.

Abstract

The synthesis of new N-homopiperazinyl-based ligands is reported. Various structural modifications along with the corresponding biological activities on 5-HT(1A)/5-HT(7) receptors give further insights into this class of serotoninergic ligands. Among the tested central heterocyles, the 7-azaindole gave the best results on the above-mentioned receptors.

MeSH terms

  • Drug Design
  • Humans
  • Indoles
  • Ligands
  • Piperazine
  • Piperazines / chemical synthesis
  • Piperazines / chemistry*
  • Piperazines / pharmacology
  • Protein Binding
  • Radioligand Assay
  • Receptor, Serotonin, 5-HT1A
  • Receptors, Serotonin
  • Serotonin Receptor Agonists / chemical synthesis
  • Serotonin Receptor Agonists / chemistry*
  • Structure-Activity Relationship

Substances

  • 7-azaindole dimer
  • Indoles
  • Ligands
  • Piperazines
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • serotonin 7 receptor
  • Receptor, Serotonin, 5-HT1A
  • Piperazine