Amino-3,5-Dicyanopyridines Targeting the Adenosine Receptors Ranging from Pan Ligands to Combined A₁/A_2B Partial Agonists.

ABSTRACT: The amino-3,5-dicyanopyridine derivatives belong to an intriguing series of adenosine receptor (AR) ligands that has been developed by both academic researchers and industry. Indeed, the studies carried out to date underline the versatility of the dicyanopyridine scaffold to obtain AR ligands with not only a wide range of affinities but also with diverse degrees of efficacies at the different ARs. These observations prompted us to investigate on the structure-activity relationships (SARs) of this series leading to important previously reported results. The present SAR study has helped to confirm the 1H-imidazol-2-yl group at R² position as an important feature for producing potent AR agonists. Moreover, the nature of the R¹ substituent highly affects not only a

SUBMITTER: Catarzi D 

PROVIDER: S-EPMC6958422 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature