2, 9-Disubstituted-N 6-(arylcarbamoyl)-8-azaadenines as new selective A 3 adenosine receptor antagonists: synthesis, biochemical and molecular modelling studies

…, L Fabbrini, I Giorgi, O Livi, I Micco, F Pacchini…

Index: Biagi, Giuliana; Bianucci, Anna Maria; Coi, Alessio; Costa, Barbara; Fabbrini, Laura; Giorgi, Irene; Livi, Oreste; Micco, Iolanda; Pacchini, Federica; Santini, Edoardo; Leonardi, Michele; Nofal, Fatena Ahmad; Salerni, Oreste LeRoy; Scartoni, Valerio Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 15 p. 4679 - 4693

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Citation Number: 26

Abstract

A number of N6-(N-arylcarbamoyl)-2-substituted-9-benzyl-8-azaadenines, obtained by a modification of the synthetic scheme used to prepare selective A1 ligands, by only three or two steps, are described. At first we prepared a series of 2-phenyl-9-benzyl-8-azaadenines having as N6 substituent a variously substituted N-phenylcarbamoyl group. Some of these derivatives demonstrated good affinity towards the A3 subtype but low selectivity. ...