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A new series of 4′-selenoadenosine-5′- N,N -dimethyluronamide derivatives as highly potent and selective human A 3  adenosine receptor (hA 3 AR) antagonists, is described. The highly selective A 3 AR agonists, 4′-selenoadenosine-5′- N -methyluronamides were successfully converted into selective antagonists by adding a second  N -methyl group to the 5′-uronamide position. All the synthesized compounds showed medium to high binding affinity at the hA 3 AR. Among the synthesized compounds, 2-H- N  6 -3-iodobenzylamine derivative  9f  exhibited the highest binding affinity at hA 3 AR. ( K i   = 22.7 nM). The 2-H analogues generally showed better binding affinity than the 2-Cl analogues. The cAMP functional assay with 2-Cl- N  6 -3-iodobenzylamine derivative  9l  demonstrated hA 3 AR antagonist activity. A molecular modelling study suggests an important role of the hydrogen of 5′-uronamide as an essential hydrogen bonding donor for hA 3 AR activation.

Design and Synthesis of 2,6-Disubstituted-4′-Selenoadenosine-5′-N,N-Dimethyluronamide Derivatives as Human A3 Adenosine Receptor Antagonists