title: Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
abstract: We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.
authors.affiliation: Vernalis (R&D) Ltd, 613 Reading Road, Winnersh, Wokingham 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: Paul R
authors.initials: PR
authors.lastname: Giles
authors.forename: Allan M
authors.initials: AM
authors.lastname: Jordan
authors.forename: Antony R
authors.initials: AR
authors.lastname: Knight
authors.forename: Anthony
authors.initials: A
authors.lastname: Lawrence
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: Richard S
authors.initials: RS
authors.lastname: Todd
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; D058918:Adenosine A3 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*; 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; D058918:Adenosine A3 Receptor Antagonists; D000978:Antiparkinson Agents; D011743:Pyrimidines