Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
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.
Gillespie
Roger J
RJ
Vernalis (R&D) Ltd, 613 Reading Road, Winnersh, Wokingham RG41 5UA, UK.
Cliffe
Ian A
IA
Dawson
Claire E
CE
Dourish
Colin T
CT
Gaur
Suneel
S
Giles
Paul R
PR
Jordan
Allan M
AM
Knight
Antony R
AR
Lawrence
Anthony
A
Lerpiniere
Joanne
J
Misra
Anil
A
Pratt
Robert M
RM
Todd
Richard S
RS
Upton
Rebecca
R
Weiss
Scott M
SM
Williamson
Douglas S
DS
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
D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D058918:Adenosine A3 Receptor Antagonists; D000978:Antiparkinson Agents; D011743:Pyrimidines