Ribose-modified adenosine analogs as potential partial agonists for the adenosine receptor

…, JK von Frijtag Drabbe Kuenzel…

Index: Van der Wenden; Von Frijtag Drabbe Kunzel; Mathot; Danhof; Ijzerman; Soudijn Journal of Medicinal Chemistry, 1995 , vol. 38, # 20 p. 4000 - 4006

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Citation Number: 91

Abstract

We have adopted a practical three-step route for the synthesis of 2'-and 3'-deoxy analogues of N6-substituted adenosines: protection of the hydroxyl groups, replacement of the NG- amino by a better leaving group, and combined deprotection and N6-amination in the last step. This route was used to synthesize deoxy analogues of CPA, CHA, and R-and S-PIA. The compounds were tested on the adenosine A1 and Aza receptors in our search for ...