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Antagonists of the human adenosine A(2A) receptor. Part 1: Discovery and synthesis of thieno[3,2-d] pyrimidine-4-methanone derivatives
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posted on 2023-06-08, 05:20 authored by Simon WardThe (-)-(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
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Publication status
- Published
Journal
Bioorganic and Medicinal Chemistry LettersISSN
0960894XPublisher
ElsevierExternal DOI
Issue
9Volume
18Page range
2916-2919Department affiliated with
- Chemistry Publications
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- No
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- Yes
Legacy Posted Date
2012-02-06Usage metrics
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