title: Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists.
abstract: Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route, of A2A receptor antagonists containing the [1,2,4]triazolo[1,5-a]pyrazine nucleus, which is isomeric with the [1,2,4]triazolo[1,5-c]pyrimidine core of a series of known A2A antagonists with in vivo activity in animal models of Parkinson's disease.
authors.affiliation: Biogen Idec, Inc., 14 Cambridge Center, Cambridge, MA 02142, USA. james.dowling@biogenidec.com
authors.forename: James E
authors.initials: JE
authors.lastname: Dowling
authors.forename: Jeffrey T
authors.initials: JT
authors.lastname: Vessels
authors.forename: Serajul
authors.initials: S
authors.lastname: Haque
authors.forename: He Xi
authors.initials: HX
authors.lastname: Chang
authors.forename: Kurt
authors.initials: K
authors.lastname: van Vloten
authors.forename: Gnanasambandam
authors.initials: G
authors.lastname: Kumaravel
authors.forename: Thomas
authors.initials: T
authors.lastname: Engber
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Jin
authors.forename: Deepali
authors.initials: D
authors.lastname: Phadke
authors.forename: Joy
authors.initials: J
authors.lastname: Wang
authors.forename: Eman
authors.initials: E
authors.lastname: Ayyub
authors.forename: Russell C
authors.initials: RC
authors.lastname: Petter
mesh_terms: D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D001921:Brain / Q000648:ultrastructure; D002462:Cell Membrane / Q000737:chemistry / Q000378:metabolism; D004195:Disease Models, Animal; D010300:Parkinson Disease / Q000188:drug therapy; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D011719:Pyrazines