Synthesis and Biological Evaluation of Novel 1-Deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]-9H-purin-9-yl]-N-ethyl-β-d-ribofuranuronamide Derivatives as Useful Templates for theDevelopment of A2B Adenosine Receptor Agonists
The lack of molecules endowed with selective and potent agonistic activity toward the hA2B adenosinereceptors has limited the studies on this pharmacological target and consequently the evaluation of itstherapeutic potential. We report the design and the synthesis of the first potent (EC50 in the nanomolarrange) and selective hA2B adenosine receptor agonists consisting of 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]-9H-purin-9-yl]-N-ethyl-β-d-ribofuranuronamide derivatives. The concurrent effect of 6-substitutionof the purine nucleus with a ((hetero)arylcarbonyl)hydrazino function and a 2-chloro substitution has beeninvestigated in such NECA derivatives.
