title: Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones.
abstract: Antagonism of the adenosine A(2A) receptor affords a possible treatment of Parkinson's disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A(1)) A(2A) antagonist activity. Structure-activity relationships are described for this series.
authors.affiliation: Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. joel.harris@merck.com
authors.forename: Joel M
authors.initials: JM
authors.lastname: Harris
authors.forename: Bernard R
authors.initials: BR
authors.lastname: Neustadt
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
authors.forename: Jean
authors.initials: J
authors.lastname: Lachowicz
authors.forename: Mary
authors.initials: M
authors.lastname: Cohen-Williams
authors.forename: Geoff
authors.initials: G
authors.lastname: Varty
authors.forename: Jinsong
authors.initials: J
authors.lastname: Hao
authors.forename: Andrew W
authors.initials: AW
authors.lastname: Stamford
mesh_terms: D058917:Adenosine A2 Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D043705:Receptor, Adenosine A2A / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D011744:Pyrimidinones; D043705:Receptor, Adenosine A2A