Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers

A number of 2-aminothiazoles (2a–e) and their amide derivatives (4–10) were prepared. The 2-aminothiazoles themselves were tested as allosteric enhancers of agonist binding to human adenosine A1 receptors. In a variety of experimental set-ups the compounds did not show any such effect, in contrast to earlier findings by another research group. Subsequently the 2-aminothiazoles were used as intermediates in the synthesis of a number of amide derivatives of either aromatic (4–6) or aliphatic nature (7–10). Some of the compounds emerged as moderately active antagonists on human adenosine A1 and/or A2A receptors with lower or negligible potency at adenosine A3 receptors.

Figure optionsDownload as PowerPoint slide