We recently described the synthesis of 1-benzyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-diones, new potent and selective A(3) adenosine receptor antagonists containing a xanthine core. The present work can be considered an extension of our SAR studies on related structures in which the effect of different kind of substitutions at the 1-, 3- and 8-positions has been evaluated in order to improve both the potency and the hydrophilicity of the originally synthesised molecules. The A(3) binding disposition of these compounds was also investigated through docking and 3D-QSAR studies.
|Autori:||BARALDI PIER GIOVANNI; PRETI DELIA; TABRIZI MOJGAN AGHAZADEH; ROMAGNOLI ROMEO; SAPONARO GIULIA; BARALDI STEFANIA; BOTTA MAURIZIO; BERNARDINI CESARE; TAFI ANDREA; TUCCINARDI TIZIANO; MARTINELLI A; VARANI KATIA; BOREA PIER ANDREA|
|Titolo:||Structure-Activity Relationship Studies of a New Series of Imidazo2,1-fpurinones as Potent and Selective A3 Adenosine Receptor Antagonists|
|Anno del prodotto:||2008|
|Digital Object Identifier (DOI):||10.1016/j.bmc.2008.10.049|
|Appare nelle tipologie:||1.1 Articolo in rivista|