Press, Neil, Taylor, Roger, Fullerton, Joe, Tranter, Pamela, Mccarthy, Clive, Keller, Thomas, Brown, Lyndon, Cheung, Robert, Christie, Julie, Haberthuer, Sandra, Hatto, Julia, Keenan, Mark, Mercer, Mark, Press, Nicola, Sahri, Helene, Tuffnell, Andrew, Tweed, Morris and Fozard, John R. (2005) A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential. Bioorganic & Medicinal Chemistry Letters, 15 (12). pp. 3081-3085. ISSN 0960-894X

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.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.04.021
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	Adenosine; A2B; A3; Adenosine receptor antagonist; Asthma; Aminothiazole
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.04.021
Date Deposited:	14 Dec 2009 13:56
Last Modified:	31 Jan 2013 01:11
URI:	https://oak.novartis.com/id/eprint/640