title: Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
abstract: A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.
authors.affiliation: Vernalis (R&D) Ltd, 613 Reading Road, Winnersh RG41 5UA, UK.
authors.forename: Roger J
authors.initials: RJ
authors.lastname: Gillespie
authors.forename: Ian A
authors.initials: IA
authors.lastname: Cliffe
authors.forename: Claire E
authors.initials: CE
authors.lastname: Dawson
authors.forename: Colin T
authors.initials: CT
authors.lastname: Dourish
authors.forename: Suneel
authors.initials: S
authors.lastname: Gaur
authors.forename: Allan M
authors.initials: AM
authors.lastname: Jordan
authors.forename: Antony R
authors.initials: AR
authors.lastname: Knight
authors.forename: Joanne
authors.initials: J
authors.lastname: Lerpiniere
authors.forename: Anil
authors.initials: A
authors.lastname: Misra
authors.forename: Robert M
authors.initials: RM
authors.lastname: Pratt
authors.forename: Jonathan
authors.initials: J
authors.lastname: Roffey
authors.forename: Gemma C
authors.initials: GC
authors.lastname: Stratton
authors.forename: Rebecca
authors.initials: R
authors.lastname: Upton
authors.forename: Scott M
authors.initials: SM
authors.lastname: Weiss
authors.forename: Douglas S
authors.initials: DS
authors.lastname: Williamson
mesh_terms: D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D015195:Drug Design; D006801:Humans; D008956:Models, Chemical; D020734:Parkinsonian Disorders / Q000188:drug therapy*; D011687:Purines / Q000138:chemical synthesis / Q000627:therapeutic use*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000627:therapeutic use*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000627:therapeutic use*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D011687:Purines; D011720:Pyrazoles; D011743:Pyrimidines