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Bioorg Med Chem Lett. 2005 Jun 15;15(12):3081-5.

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

Author information

1
Novartis Institutes for Biomedical Research, Respiratory Diseases Area, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK. neil.press@novartis.com

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.

PMID:
15876531
DOI:
10.1016/j.bmcl.2005.04.021
[Indexed for MEDLINE]

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