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The (-)-(11R,2'S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A(2A) receptor antagonist. Further investigation of this compound has led to the discovery of a series of keto-aryl thieno[3,2-d]pyrimidine derivatives, which are potent and selective antagonists of the adenosine A(2A) receptor. These derivatives show selectivity against the A(1) receptor. Furthermore, some of these compounds have been shown to have in vivo activity in a commonly used model, suggesting the potential for the treatment of Parkinson's disease.

Original publication

DOI

10.1016/j.bmcl.2008.03.075

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/05/2008

Volume

18

Pages

2916 - 2919

Keywords

Adenosine A2 Receptor Antagonists, Antimalarials, Antiparkinson Agents, Humans, Models, Chemical, Parkinsonian Disorders, Pyrimidines, Stereoisomerism, Structure-Activity Relationship