title: Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
abstract: Piperazine and (R)-2-(aminomethyl)pyrrolidine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been shown to be potent and selective adenosine A(2a) receptor antagonists. We have replaced the triazolotriazine core structure with two different heterocyclic cores. One of these, the one deriving from [1,2,4]triazolo[1,5-c]pyrimidine, appears to be particularly effective and selected analogs from this series have been shown to be orally active in a mouse catalepsy model of Parkinson's disease.
authors.affiliation: Biogen Idec, Inc., Department of Medicinal Chemistry, 14 Cambridge Center, Cambridge, MA 02142, USA. chi.vu@biogenidec.com
authors.forename: Chi B
authors.initials: CB
authors.lastname: Vu
authors.forename: Deborah
authors.initials: D
authors.lastname: Pan
authors.forename: Bo
authors.initials: B
authors.lastname: Peng
authors.forename: Li
authors.initials: L
authors.lastname: Sha
authors.forename: Gnanasambandam
authors.initials: G
authors.lastname: Kumaravel
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Jin
authors.forename: Deepali
authors.initials: D
authors.lastname: Phadke
authors.forename: Thomas
authors.initials: T
authors.lastname: Engber
authors.forename: Carol
authors.initials: C
authors.lastname: Huang
authors.forename: Jennifer
authors.initials: J
authors.lastname: Reilly
authors.forename: Stacy
authors.initials: S
authors.lastname: Tam
authors.forename: Russell C
authors.initials: RC
authors.lastname: Petter
mesh_terms: D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology*; D002375:Catalepsy / Q000188:drug therapy; D051379:Mice; D011743:Pyrimidines / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000494:pharmacology
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D011743:Pyrimidines; D014230:Triazoles