2-Aminothiazoles: A new class of agonist allosteric enhancers of A 1 adenosine receptors

…, LJ Murphree, TL Macdonald, J Linden…

Index: Chordia, Mahendra D.; Murphree, Lauren J.; Macdonald, Timothy L.; Linden, Joel; Olsson, Ray A. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 12 p. 1563 - 1566

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Citation Number: 38

Abstract

This report describes the synthesis and structure–activity relationships of a new class of A1 adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC50 of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 μM, substantially lower than that of the 'Gold Standard'2-amino-3-benzoyl thiophene (PD 81,723), which has an EC50 of 38 μM.