A solid phase parallel synthesis of diverse amides as dopamine D3 receptor ligands

J Enzyme Inhib Med Chem. 2008 Oct;23(5):588-92. doi: 10.1080/14756360701830023.

Abstract

A solid phase parallel synthesis using SynPhase technology was used to couple a series of 21 carboxylic with three different 4-(4-arylpiperazinyl)butanamines. The resulting library was evaluated as dopamine D(3) receptor ligands giving rise to several compounds with affinities in the low nanomolar concentration range (9e and 9n with binding affinities at D(3) receptors of 0.10 and 0.35 nM respectively).

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Amines / chemistry
  • Animals
  • Carboxylic Acids / chemistry
  • Humans
  • Ligands
  • Receptors, Dopamine D3 / chemistry*
  • Small Molecule Libraries / chemical synthesis*

Substances

  • Amides
  • Amines
  • Carboxylic Acids
  • Ligands
  • Receptors, Dopamine D3
  • Small Molecule Libraries