| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379722 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
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.
Graphical abstractThe 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 full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Neil J. Press, Roger J. Taylor, Joseph D. Fullerton, Pamela Tranter, Clive McCarthy, Thomas H. Keller, Lyndon Brown, Robert Cheung, Julie Christie, Sandra Haberthuer, Julia D.I. Hatto, Mark Keenan, Mark K. Mercer, Nicola E. Press, Helene Sahri,