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.
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.
Gillespie
Roger J
RJ
Vernalis (R&D) Ltd, 613 Reading Road, Winnersh RG41 5UA, UK.
Cliffe
Ian A
IA
Dawson
Claire E
CE
Dourish
Colin T
CT
Gaur
Suneel
S
Jordan
Allan M
AM
Knight
Antony R
AR
Lerpiniere
Joanne
J
Misra
Anil
A
Pratt
Robert M
RM
Roffey
Jonathan
J
Stratton
Gemma C
GC
Upton
Rebecca
R
Weiss
Scott M
SM
Williamson
Douglas S
DS
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
D058916:Adenosine A1 Receptor Antagonists; D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D011687:Purines; D011720:Pyrazoles; D011743:Pyrimidines