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ID: ALA1135449

Journal: Bioorg Med Chem Lett

Title: A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: binding activity at D2 and D3 receptors.

Authors: Dutta AK, Fei XS, Reith ME.

Abstract: A series of 7-hydroxy-2-[N-alkyl-(N-(4-phenylpiperazine)-alkyl)amino]tetralins was developed based on a novel hybrid approach that combined 2-aminotetralin and arylpiperazine pharmacophoric moieties. Our preliminary study revealed that a four-methylene butyl linker produced very potent compounds for both the D2 and D3 receptors. Further structure-activity studies led to a novel template showing 50- to 100-fold selectivity for the D3 receptor.

CiteXplore: 11844685

DOI: 10.1016/s0960-894x(01)00820-4