Structure-Activity Relationships of 2, N 6, 5'-Substituted Adenosine Derivatives with Potent Activity at the A2B Adenosine Receptor

…, KK Palaniappan, AA Ivanov, N Bergman…

Index: Adachi, Hayamitsu; Palaniappan, Krishnan K.; Ivanov, Andrei A.; Bergman, Nathaniel; Gao, Zhan-Guo; Jacobson, Kenneth A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 8 p. 1810 - 1827

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Citation Number: 35

Abstract

2, N 6, and 5'-substituted adenosine derivatives were synthesized via alkylation of 2- oxypurine nucleosides leading to 2-arylalkylether derivatives. 2-(3-(Indolyl) ethyloxy) adenosine 17 was examined in both binding and cAMP assays and found to be a potent agonist of the human A2BAR. Simplification, altered connectivity, and mimicking of the indole ring of 17 failed to maintain A2BAR potency. Introduction of N 6-ethyl or N 6- ...