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

Brown, Lyndon; Cheung, Robert; Christie, Julie; Fozard, John R.; Fullerton, Joe; Haberthuer, Sandra; Hatto, Julia; Keenan, Mark; Keller, Thomas; Mccarthy, Clive; Mercer, Mark; Press, Neil; Press, Nicola; Sahri, Helene; Taylor, Roger; Tranter, Pamela; Tuffnell, Andrew; Tweed, Morris

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

Authors: Lyndon Brown
Robert Cheung
Julie Christie
John R. Fozard
Joe Fullerton
Sandra Haberthuer
Julia Hatto
Mark Keenan
Thomas Keller
Clive Mccarthy
Mark Mercer
Neil Press
Nicola Press
Helene Sahri
Roger Taylor
Pamela Tranter
Andrew Tuffnell
Morris Tweed
Publication date: 1 January 2005
Publisher: 'Elsevier BV'

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

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