New N 6-or N (9)-hydroxyalkyl substituted 8-azaadenines or adenines as effective A 1 adenosine receptor ligands

…, F Pacchini, V Scartoni, B Costa, A Lucacchini

文献索引：Biagi, Giuliana; Giorgi, Irene; Leonardi, Michele; Livi, Oreste; Pacchini, Federica; Scartoni, Valerio; Costa, Barbara; Lucacchini, Antonio European journal of medicinal chemistry, 2003 , vol. 38, # 9 p. 801 - 810

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被引用次数: 10

摘要

In this paper we describe synthesis and biological assays of some A1 ligands more water- soluble than the effective, but very lipophilic, 8-azaadenines and adenines discovered in the past and obtained introducing on N6 or N (9) substituent a hydroxy group. Five of the new N6-hydroxyalkyl-and N6-hydroxycycloalkyl-2-phenyl-9-benzyl-8-azaadenines showed very high affinity (Ki< 40 nM) and selectivity for A1 adenosine receptors. Among the 2-phenyl-9 ...