Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands:: Structure-activity relationship elucidation

被引：15
|
作者：
Peters, Jens-Uwe [1 ]
Luebbers, Thomas [1 ]
Alanine, Alexander [1 ]
Kolczewski, Sabine [1 ]
Blasco, Francesca [2 ]
Steward, Lucinda [3 ]
机构：
[1] F Hoffmann La Roche & Co Ltd, Div Pharma, Discovery Chem, CH-4070 Basel, Switzerland
[2] F Hoffmann La Roche & Co Ltd, Div Pharma, Safety Tech Serv, CH-4070 Basel, Switzerland
[3] F Hoffmann La Roche & Co Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期
关键词：
5-HT; GPCR; SAR; guanidine;
D O I：
10.1016/j.bmcl.2007.10.080
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The optimisation of affinity and selectivity in a novel series of dual 5-HT5A/5-HT7 receptor ligands is described. Brain penetrant 2-aminodihydroquinazolines with low nanomolar affinities were identified. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：256 / 261
页数：6
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