Synthesis of N6-Substituted 3′-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor

Abstract

Several N6-substituted 3′-ureidoadenosine derivatives were efficiently synthesized starting from D-glucose for the development of H272E mutant A3 adenosine receptor (AR) agonists. Among compounds tested, 3′-ureido-N6-(3-iodobenzyl)adenosine (2c) exhibited the highest binding affinity (Ki = 0.22 μ M) at the H272E mutant A3 AR without binding to the natural A3AR. Copyright © Taylor & Francis Group, LLC.