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

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 D₃ receptor ligands giving rise to several compounds with affinities in the low nanomolar concentration range (9e and 9n with binding affinities at D₃ receptors of 0.10 and 0.35 nM respectively).

• D₃ receptors
• ligand
• dopamine
• amide

Acknowledgements

We gratefully acknowledge Philippe Jéhan and Marcel Morvan for technical assistance.