title: Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
abstract: Piperazine derivatives of 2-furanyl[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 now demonstrate that potent and selective A(2a) receptor antagonists could still be obtained when the arylpiperazines are separated from the triazolotriazine core structure by an ethylenediamine spacer. Selected analogs bearing this triazolotriazine or the related triazolopyrimidine core structure have been found 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: Pamela
authors.initials: P
authors.lastname: Shields
authors.forename: Bo
authors.initials: B
authors.lastname: Peng
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: Joy
authors.initials: J
authors.lastname: Wang
authors.forename: Thomas
authors.initials: T
authors.lastname: Engber
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; D000978:Antiparkinson Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D011743:Pyrimidines; D014227:Triazines; D014230:Triazoles