Strategically Functionalized Adenosines: Agonists for Adenosine Receptors |
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Authors: | Vasu Nair Steven A Adah Seung B Ha |
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Institution: | Department of Chemistry , University of Iowa , Iowa City, Iowa, 52242, U.S.A. |
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Abstract: | Abstract The syntheses of three classes of adenosine analogues involving cyclosubstitution at the 6-position and functionalization at the 2-position are reported. The target molecules synthesized are stable with respect to hydrolytic deamination by mammalian adenosine deaminase, and, because of major structural changes at the 2- and 6-positions, these compounds are expected to be poor phosphorylation substrates for the kinases. Adenosine receptor binding data reveal that several of the compounds synthesized show excellent A1 receptor affinity and A2/A1 selectivity. |
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