6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Structure-activity relationships have been investigated through substitutions at the 9-position of the 2-amino-6-(2-furanyl) purine (5) to identify novel and selective A(2A) adenosine receptor antagonists. Several potent and selective antagonists were identified. In particular, compounds 20, 25, and 26 show very high affinity with excellent selectivity.
Kiselgof
Eugenia
E
Schering-Plough Research Institute, Chemical Research, 2015 Galloping Hill Road, MS 2545, Kenilworth, NJ 07033, USA.
Tulshian
Deen B
DB
Arik
Leyla
L
Zhang
Hongtao
H
Fawzi
Ahmad
A
D058917:Adenosine A2 Receptor Antagonists; D002460:Cell Line; D006801:Humans; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D011743:Pyrimidines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D043705:Receptor, Adenosine A2A / Q000378:metabolism / Q000502:physiology; D014230:Triazoles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*
C098657:5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine; D058917:Adenosine A2 Receptor Antagonists; D011743:Pyrimidines; D043705:Receptor, Adenosine A2A; D014230:Triazoles