Il Farmaco

erythro-and threo-2-Hydroxynonyl substituted 2-phenyladenines and 2-phenyl-8-azaadenines: ligands for A 1 adenosine receptors and adenosine deaminase

…, I Giorgi, O Livi, F Pacchini, P Rum, V Scartoni, B Costa…

文献索引：Biagi, Giuliana; Giorgi, Irene; Livi, Oreste; Pacchini, Federica; Rum, Pietro; Scartoni, Valerio; Costa, Barbara; Mazzoni, Maria Rosa; Giusti, Laura Farmaco, 2002 , vol. 57, # 3 p. 221 - 233

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被引用次数: 14

摘要

erythro-2-Phenyl-9-(2-hydroxy-3-nonyl) adenine and its 8-aza analog were prepared and showed a very high inhibitory activity towards adenosine deaminase (ADA), with Ki 0.55 and 1.67 nM, respectively, and high affinity for A1 adenosine receptors, with Ki 28 and 2.8 nM, respectively. To increase affinity for A1 receptors we introduced a substituent on the N6 position such as alkyl or cycloalkyl groups, which are present in effective agonists or ...