title: 6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
abstract: 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.
authors.affiliation: Schering-Plough Research Institute, Chemical Research, 2015 Galloping Hill Road, MS 2545, Kenilworth, NJ 07033, USA.
authors.forename: Eugenia
authors.initials: E
authors.lastname: Kiselgof
authors.forename: Deen B
authors.initials: DB
authors.lastname: Tulshian
authors.forename: Leyla
authors.initials: L
authors.lastname: Arik
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
authors.forename: Ahmad
authors.initials: A
authors.lastname: Fawzi
mesh_terms: 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*
chemical_list: 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