SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as μ opioid ligands

被引：9

作者：

Lunn, Graham ^{[1
]}

Roberts, Lee R. ^{[1
]}

Content, Stephane ^{[1
]}

Critcher, Douglas J. ^{[1
]}

Douglas, Sara ^{[1
]}

Fenwick, Ashley E. ^{[1
]}

Gethin, David M. ^{[1
]}

Goodwin, Graham ^{[1
]}

Greenway, David ^{[1
]}

Greenwood, Sean ^{[1
]}

Hall, Kim ^{[1
]}

Thomas, Martin ^{[1
]}

Thompson, Stephen ^{[1
]}

Williams, David ^{[1
]}

Wood, Gavin ^{[1
]}

Wylie, Andrew ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Sandwich Labs, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 06期

关键词：

mu Opioid; Opioid; RECEPTOR ANTAGONIST; DISCOVERY; PRURITUS;

D O I：

10.1016/j.bmcl.2012.01.099

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

3-Azabicyclo[3.1.0] hexane compounds were designed as novel achiral mu opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which led to compounds having picomolar binding affinity, selective for the mu receptor over delta and kappa subtypes. Some subtleties of functional activity will also be described. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2200 / 2203

页数：4

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