The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles

Article abstract of DOI:10.1016/S0960-894X(98)00302-3

The synthesis and purinergic receptor binding of novel adenosine A₃ ligands is described. Many selective A₃ receptor agonists e.g. N-(3- iodobenzyl)adenosine-5'-methyluronamide (IB-MECA) contain a 4'- ribosylalkylamide moiety. We found that this amide and other 4'-functional groups could be replaced with an isosteric isoxazole, and the target molecules retained potent binding to the recombinant human A₃ receptor.