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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2008-05, Vol.18 (9), p.2924-2929
Main Authors: GILLESPIE, Roger J, CLIFFE, Ian A, ROLFEY, Jonathan, STRATTON, Gemma C, UPTON, Rebecca, WEISS, Scott M, WILLIAMSON, Douglas S, DAWSON, Claire E, DOURISH, Colin T, GAUR, Suneel, JORDAN, Allan M, KNIGHT, Antony R, LERPINIERE, Joanne, MISRA, Anil, PRATT, Robert M
Format: Article
Language:English
Subjects:
Adenosine A1 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Anticonvulsants. Antiepileptics. Antiparkinson agents
Antiparkinson Agents - chemical synthesis
Antiparkinson Agents - therapeutic use
Biological and medical sciences
Drug Design
Humans
Medical sciences
Models, Chemical
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Parkinsonian Disorders - drug therapy
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Purines - chemical synthesis
Purines - therapeutic use
Pyrazoles - chemical synthesis
Pyrazoles - therapeutic use
Pyrimidines - chemical synthesis
Pyrimidines - therapeutic use
Stereoisomerism
Structure-Activity Relationship
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.03.072