Potent and selective adenosine A₂A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

Antagonism of the adenosine A₂A receptor affords a possible treatment of Parkinson’s disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A₂A antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A₁) A₂A antagonist activity....

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (8), p.2497-2501
Main Authors: Harris, Joel M, Neustadt, Bernard R, Zhang, Hongtao, Lachowicz, Jean, Cohen-Williams, Mary, Varty, Geoff, Hao, Jinsong, Stamford, Andrew W
Format: Article
Language:English
Subjects:
antagonists
Biological and medical sciences
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Parkinson disease
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
structure-activity relationships
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Summary:Antagonism of the adenosine A₂A receptor affords a possible treatment of Parkinson’s disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A₂A antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A₁) A₂A antagonist activity. Structure–activity relationships are described for this series.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.02.045