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发现并优化高效且选择性的人源腺苷 A2B 受体功能拮抗剂。

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

机构信息

Vernalis (R&D) Ltd, Granta Park, Cambridge, CB21 6GB, UK.

出版信息

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5945-9. doi: 10.1016/j.bmcl.2009.08.040. Epub 2009 Aug 14.

DOI:10.1016/j.bmcl.2009.08.040
PMID:19733067
Abstract

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.

摘要

我们在此报告了一种新型人类腺苷 A2B 受体拮抗剂的发现。这个低分子量支架已经过优化，以提供具有缓解与该受体亚型相关的疾病（如疼痛、糖尿病、哮喘和 COPD）潜力的衍生物。此外，初步的药代动力学分析显示，这些化合物具有适合吸入或全身给药途径的特征。

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