A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential

The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.

The synthesis and SAR of novel aminothiazoles as adenosine receptor antagonists is described, culminating in the synthesis of a potent and orally bioavailable dual A2B/A3 receptor antagonist.Figure optionsDownload as PowerPoint slide