Discovery and Structure-Activity Relationship Studies of Novel Adenosine A₁ Receptor-Selective Agonists.

ABSTRACT: A series of benzyloxy and phenoxy derivatives of the adenosine receptor agonists N⁶-cyclopentyl adenosine (CPA) and N⁶-cyclopentyl 5'-N-ethylcarboxamidoadenosine (CP-NECA) were synthesized, and their potency and selectivity were assessed. We observed that the most potent were the compounds with a halogen in the meta position on the aromatic ring of the benzyloxy- or phenoxycyclopentyl substituent. In general, the NECA-based compounds displayed greater A₁R selectivity than the adenosine-based compounds, with N⁶-2-(3-bromobenzyloxy)cyclopentyl-NECA and N⁶-2-(3-methoxyphenoxy)cyclopentyl-NECA showing ∼1500-fold improved A₁R selectivity compared to NECA. In addition, we quantified the co

SUBMITTER: Preti B 

PROVIDER: S-EPMC9661479 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature