Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor

被引：9

作者：

Bedford, Simon T. ^{[1
]}

Benwell, Karen R. ^{[1
]}

Brooks, Teresa ^{[1
]}

Chen, Ijen ^{[1
]}

Comer, Mike ^{[2
]}

Dugdale, Sarah ^{[2
]}

Haymes, Tim ^{[2
]}

Jordan, Allan M. ^{[1
]}

Kennett, Guy A. ^{[2
]}

Knight, Anthony R. ^{[2
]}

Klenke, Burkhard ^{[2
]}

LeStrat, Loic ^{[1
]}

Merrett, Angela ^{[2
]}

Misra, Anil ^{[2
]}

Lightowler, Sean ^{[2
]}

Padfield, Anthony ^{[2
]}

Poullennec, Karine ^{[2
]}

Reece, Mark ^{[2
]}

Simmonite, Heather ^{[1
]}

Wong, Melanie ^{[1
]}

Yule, Ian A. ^{[2
]}

机构：

[1] Vernalis R&D Ltd, Cambridge CB21 6GB, England

[2] Vernalis R&D Ltd, Winnersh RG41 5UA, Wokingham, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 20期

关键词：

Adenosine receptor; Functional antagonist; Asthma; COPD; AQUEOUS SOLUBILITY; HIGHLY POTENT; DERIVATIVES; DESIGN;

D O I：

10.1016/j.bmcl.2009.08.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We herein report the discovery of a novel class of antagonists of the human adenosine A2B receptor. This low molecular weight scaffold has been optimized to offer derivatives with potential utility for the alleviation of conditions associated with this receptor subtype, such as nociception, diabetes, asthma and COPD. Furthermore, preliminary pharmacokinetic analysis has revealed compounds with profiles suitable for either inhaled or systemic routes of administration. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5945 / 5949

页数：5

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