N6-SUBSTITUTED ADENOSINE RECEPTOR AGONISTS : POTENTIAL ANTIHYPERTENSIVE AGENTS

Preparation a series of novel N 6 -benzocycloalkyladenosines and studied their receptor binding and antihypertensive activity. The structure-activity relationship study shows that the adenosine analogues having the hydrophobic phenyl moiety one carbon away from the C6-nitrogen have modest affinity and selectivity for the A 1 receptor, whereas those with the phenyl moiety two carbons away from the C6-nitrogen have excellent affinity and selectivity for the A 1 receptor. Many of these analogues showed excellent antihypertensive activity with a wide range of effects on heart rate