A new class of potent non-imidazole H3 antagonists:: 2-aminoethylbenzofurans

被引：80

作者：

Cowart, M ^{[1
]}

Pratt, JK ^{[1
]}

Stewart, AO ^{[1
]}

Bennani, YL ^{[1
]}

Esbenshade, TA ^{[1
]}

Hancock, AA ^{[1
]}

机构：

[1] Abbott Labs, Dept Neurosci Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.11.032

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Aminoethylbenzofurans constitute a new class of H-3 antagonists that are more rotationally constrained than most previously reported H-3 antagonists. They retain high potency at human and rat receptors, with efficient CNS penetration observed in 35. The SAR of the basic amine moiety was compared in three different series of analogues. The greatest potency was found in analogues bearing a 2-methylpyrrolidine, a 2,5-dimethylpyrrolidine, or a 2,6-dimethylpiperidine. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：689 / 693

页数：5

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