Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides:: Novel and selective histamine H3 receptor antagonists

被引:46
作者
Faghih, R [1 ]
Dwight, W [1 ]
Pan, JB [1 ]
Fox, GB [1 ]
Krueger, KM [1 ]
Esbenshade, TA [1 ]
McVey, JM [1 ]
Marsh, K [1 ]
Bennani, YL [1 ]
Hancock, AA [1 ]
机构
[1] Abbott Labs, Global Pharmaceut Res & Dev, Neurosci Res, Abbott Pk, IL 60064 USA
关键词
D O I
10.1016/S0960-894X(03)00118-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel 4'-[(NRIR2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H(3)receptors. Most compounds were highly potent and selective for human and rat H-3 receptors and selected examples such as A-349821 showed functional antagonism of H3 receptors in vitro and in a mouse dipsogenia model. (C) 2003 Published by Elsevier Science Ltd.
引用
收藏
页码:1325 / 1328
页数:4
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