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Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists

, : Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists. Journal of Medicinal Chemistry 48(5): 1550-1562

A number of 3'-C-methyl analogues of selective adenosine receptor agonists such as CPA, CHA, CCPA, 2'-Me-CCPA, NECA, and IB-MECA was synthesized to further investigate the subdomain of the receptor that binds the ribose moiety of the ligands. Affinity data at A1, A2A, and A3 receptors in bovine brain membranes showed that the X-C-modification in adenosine resulted in a decrease of the affinity at all three receptor subtypes.


PMID: 15743197

DOI: 10.1021/jm049408n

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