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A solid phase parallel synthesis of diverse amides as dopamine D3 receptor ligands
Authors:Jean Mickaël  Renault Jacques  Camelin Jean-Claude  Levoin Nicolas  Danvy Denis  Stark Holger  Capet Marc  Uriac Philippe
Affiliation:UPRES EA 4090, Substances licheniques et photoprotection, Faculte des Sciences Biologiques et Medicales, Universite de Rennes I, Rennes, France.
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).
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