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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.

Original publication

DOI

10.1016/j.bmcl.2008.03.076

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/05/2008

Volume

18

Pages

2920 - 2923

Keywords

Adenosine A1 Receptor Antagonists, Adenosine A2 Receptor Antagonists, Adenosine A3 Receptor Antagonists, Antiparkinson Agents, Drug Design, Humans, Models, Chemical, Parkinsonian Disorders, Pyrimidines, Stereoisomerism, Structure-Activity Relationship