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

Authors :: Press, Neil J.
Taylor, Roger J.
Fullerton, Joseph D.
Tranter, Pamela
McCarthy, Clive
Keller, Thomas H.
Brown, Lyndon
Cheung, Robert
Christie, Julie
Haberthuer, Sandra
Hatto, Julia D.I.
Keenan, Mark
Mercer, Mark K.
Press, Nicola E.
Sahri, Helene
Tuffnell, Andrew R.
Tweed, Morris
Fozard, John R.
Source :: Bioorganic & Medicinal Chemistry Letters. Jun2005, Vol. 15 Issue 12, p3081-3085. 5p.
Publication Year :: 2005
Abstract: 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. [Copyright &y& Elsevier]

Subjects :: *ADENINE
*OBSTRUCTIVE lung diseases
*RESPIRATORY allergy
*ALLERGIES

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