Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5520
Title: structure-activity relationship studies of a new series of imidazi[2,1-f]purinones as potent and selective A3 adenosine receptor antagonists
Authors: BARALDI P., G
Preti, D
TABRIZI M., A
Romagnoli, R
Saponaro, G
Baraldi, S
Botta, Maurizio 
Bernardini, C
Tafi, Andrea 
Tuccinardi, T
Martinelli, A
Varani, K
Borea, P. A.
Issue Date: 2008
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
We recently described the synthesis of 1-benzyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-diones, new potent and selective A3 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 A3 binding disposition of these compounds was also investigated through docking and 3D-QSAR studies.
Description: 
36560
URI: http://hdl.handle.net/20.500.12779/5520
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.10.049
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