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

2005; Elsevier BV; Volume: 15; Issue: 12 Linguagem: Inglês

10.1016/j.bmcl.2005.04.021

1464-3405

Neil J. Press, Roger Taylor, Joseph D. Fullerton, Pamela Tranter, Clive McCarthy, Thomas H. Keller, Lyndon Brown, Robert Cheung, Julie Christie, Sandra Haberthuer, Julia Hatto, Mark Keenan, Mark K. Mercer, Nicola E. Press, Helene Sahri, Andrew R. Tuffnell, Morris Tweed, John R. Fozard,

Receptor Mechanisms and Signaling

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.