2, 8-Disubstituted adenosine derivatives as partial agonists for the adenosine A 2A receptor

…, JFD Künzel, M de Groote, AP IJzerman

Index: Van Tilburg, Erica W.; Von Frijtag Drabbe Kuenzel, Jacobien; De Groote, Miriam; IJzerman, Ad P. Journal of Medicinal Chemistry, 2002 , vol. 45, # 2 p. 420 - 429

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Citation Number: 26

Abstract

Novel 2, 8-disubstituted adenosine derivatives were synthesized in good overall yields starting from 2-iodoadenosine. Binding affinities were determined for rat adenosine A1 and A2A receptors and human A3 receptors. Some compounds displayed good adenosine A2A receptor affinities, with most of the 2-(1-hexynyl)-and 2-[(E)-1-hexenyl]-substituted derivatives having Ki values in the nanomolar range. Although the introduction of an 8- ...