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

被引：39

作者：

Dutta, AK ^{[1
]}

Fei, XS

Reith, MEA

机构：

[1] Wayne State Univ, Dept Pharmaceut Sci, Detroit, MI 48202 USA

[2] Univ Illinois, Coll Med, Dept Biomed & Therapeut Sci, Peoria, IL 61605 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00820-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 7-hydroxy-2-[N-alkyl-(N-(4-pheny1piperazine)-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 D-2 and D-3 receptors. Further structure-activity studies led to a novel template showing 50- to 100-fold selectivity for the D-3 receptor. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：619 / 622

页数：4

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