کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1376565 981961 2008 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 9, 1 May 2008, Pages 2916–2919
نویسندگان
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