Parallel synthesis and biological screening of dopamine receptor ligands taking advantage of a click chemistry based BAL linker

J Comb Chem. Mar-Apr 2005;7(2):309-16. doi: 10.1021/cc049860s.


The click-chemistry-derived formyl indolyl methyl triazole (FIMT) resin 1a was evaluated for the parallel solid-phase synthesis of a series of BP-897-type arylcarboxamides. By application of a five-step sequence (including loading by reductive amination, subsequent amide coupling, deprotection, palladium-catalyzed N-arylation, and acidic cleavage), a focused library of putative dopamine D3 receptor ligands was constructed. The final products revealed good to excellent purity and were screened for binding at monoaminergic G-protein-coupled receptors when selected library members proved to show excellent binding affinity, especially toward the dopamine D3 receptor subtype.

MeSH terms

  • Amides / chemistry*
  • Combinatorial Chemistry Techniques / methods*
  • Dopamine Agonists / chemical synthesis*
  • Dopamine Agonists / chemistry
  • Dopamine Agonists / pharmacology
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / pharmacology
  • Drug Design
  • Ligands
  • Radioligand Assay
  • Receptors, Dopamine D3 / chemistry*
  • Structure-Activity Relationship


  • Amides
  • Dopamine Agonists
  • Dopamine Antagonists
  • Ligands
  • Receptors, Dopamine D3