Synthesis of N6‐Substituted 3′‐Ureidoadenosine Derivatives as Highly Potent Agonists at the Mutant A3 Adenosine Receptor

Several N 6 -substituted 3 ′-ureidoadenosine derivatives were efficiently synthesized starting from D-glucose for the development of H272E mutant A 3 adenosine receptor (AR) agonists. Among compounds tested, 3 ′-ureido-N 6 -(3-iodobenzyl)adenosine ( 2c ) exhibited the highest binding affinity (K i = 0.22 μ M) at the H272E mutant A 3 AR without binding to the natural A 3 AR.