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

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.

Graphical abstractA novel class of antagonists of the human adenosine A2B receptor is described. Offering interesting pharmacokinetic properties, these derivatives may prove useful in elucidating the role of adenosine A2B receptors in a number of human disease conditions.Figure optionsDownload full-size imageDownload as PowerPoint slide