C4-substituted 1-beta-D-ribofuranosylpyrazolo[3,4-d]pyrimidines as adenosine agonist analogues.
The synthesis of four novel C4-substituted 1-beta-D-ribofuranosylpyrazolo[3,4-d]pyrimidines is reported, and the compounds were examined as adenosine receptor agonist analogues. Neither receptor affinity nor biological activity was as potent as the purine counterparts. Adenosine agonists appear to be sensitive to modification of the purine base, with a nitrogen atom in the 7 position necessary for efficacy.
D000241:Adenosine / Q000378:metabolism; D000493:Allopurinol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001681:Biological Assay; D001921:Brain / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D011983:Receptors, Purinergic; D012263:Ribonucleosides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D011956:Receptors, Cell Surface; D011983:Receptors, Purinergic; D012263:Ribonucleosides; D000493:Allopurinol; D000241:Adenosine