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

页码：256 / 261

页数：6

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