Bioorganic & medicinal chemistry letters

A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: Binding activity at D 2 and D 3 receptors

AK Dutta, XS Fei, MEA Reith

Index: Dutta, Aloke K; Fei, XiangShu; Reith, Maarten E.A Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 4 p. 619 - 622

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Citation Number: 34

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 ...