5'-O-alkyl ethers of N, 2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors

…, J von Frijtag Drabbe Künzel, M de Groote…

文献索引：van Tilburg; van der Klein; von Frijtag Drabbe Kuenzel; de Groote; Stannek; Lorenzen; IJzerman Journal of medicinal chemistry, 2001 , vol. 44, # 18 p. 2966 - 2975

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被引用次数: 45

摘要

New N, 5'-di-and N, 2, 5'-trisubstituted adenosine derivatives were synthesized in good overall yields. Appropriate 5-O-alkyl-substituted ribose moieties were coupled to 6- chloropurine or 2, 6-dichloropurine via Vorbrüggen's glycosylation method. Subsequent amination and deprotection of the intermediates yielded compounds 18-35. Binding affinities were determined for rat adenosine A1 and A2A receptors and the human A3 receptor. The ...