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 tes...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-06, Vol.15 (12), p.3081-3085
Hauptverfasser:	PRESS, Neil J, TAYLOR, Roger J, HATTO, Julia D. I, KEENAN, Mark, MERCER, Mark K, PRESS, Nicola E, SAHRI, Helene, TUFFNELL, Andrew R, TWEED, Morris, FOZARD, John R, FULLERTON, Joseph D, TRANTER, Pamela, MCCARTHY, Clive, KELLER, Thomas H, BROWN, Lyndon, CHEUNG, Robert, CHRISTIE, Julie, HABERTHUER, Sandra
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine A2 Receptor Antagonists Adenosine A3 Receptor Antagonists Animals Biological and medical sciences Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - pharmacokinetics Heterocyclic Compounds - pharmacology Medical sciences Pharmacology. Drug treatments Rats Rats, Wistar Receptor, Adenosine A2B - metabolism Receptor, Adenosine A3 - metabolism Respiratory system Structure-Activity Relationship Thiazoles - chemical synthesis Thiazoles - pharmacokinetics Thiazoles - pharmacology
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.04.021