Title of article :
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives
Author/Authors :
Roger J. Gillespie، نويسنده , , David R. Adams، نويسنده , , David Bebbington، نويسنده , , Karen Benwell، نويسنده , , Ian A. Cliffe، نويسنده , , Claire E. Dawson، نويسنده , , Colin T. Dourish، نويسنده , , Allan Fletcher، نويسنده , , Suneel Gaur، نويسنده , , Paul R. Giles، نويسنده , , Allan M. Jordan، نويسنده , , Antony R. Knight، نويسنده , , Lars J.S. Knutsen، نويسنده , , Anthony Lawrence، نويسنده , , Joanne Lerpiniere، نويسنده , , Anil Misra، نويسنده , , Richard H.P. Porter، نويسنده , , Robert M. Pratt، نويسنده , , Robin Shepherd، نويسنده , , Rebecca Upton، نويسنده , , et al.، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
4
From page :
2916
To page :
2919
Abstract :
The (−)-(11R,2′S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A2A 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 A2A receptor. These derivatives show selectivity against the A1 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.
Keywords :
Adenosine A2A receptor , Mefloquine , Parkinson’s disease
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2008
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
799472
Link To Document :
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