5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors

M de Zwart, A Kourounakis, H Kooijman…

Index: De Zwart, Maarten; Kourounakis, Angeliki; Kooijman, Huub; Spek, Anthony L.; Link, Regina; Von Frijtag Drabbe Kuenzel, Jacobien K.; IJzerman, Ad P. Journal of Medicinal Chemistry, 1999 , vol. 42, # 8 p. 1384 - 1392

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Citation Number: 61

Abstract

Novel as well as known 5'-N-substituted carboxamidoadenosines were prepared via new routes that provided shorter reaction times and good yields. Binding affinities were determined for rat A1 and A2A receptors and human A3 receptors. EC50 values were determined for cyclic AMP production in CHO cells expressing human A2B receptors. On all receptor subtypes relatively small substituents on the carboxamido moiety were optimal. ...