Synthesis and Binding Affinity of Homologated Adenosine Analogues as A Adenosine Receptor Ligands.

Homologated analogues and of potent and selective A adenosine receptor ligands, IB-MECA and dimethyl-IB-MECA were synthesized from commercially available 1--acetyl-2,3,5-tri--benzoyl-β-d-ribofuranose () Co(CO)-catalyzed siloxymethylation as a key step. Unfortunately, homologated analogues and did not show significant binding affinities at three subtypes of adenosine receptors, indicating that free rotation, resulting from homologation, induced unfavorable interactions in the binding site of the receptor maybe due to the presence of many conformations.