کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376565 | 981961 | 2008 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives](/preview/png/1376565.png)
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.
The (−)-enantiomer of the antimalarial drug mefloquine is a potent and moderately selective antagonist of the adenosine A2A receptor. Further investigation of this compound has revealed a series of potent and selective keto-aryl thieno[3,2-d]pyrimidine derivatives which show promising activity in a commonly used model of Parkinson’s disease.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 9, 1 May 2008, Pages 2916–2919