کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587182 | 981425 | 2012 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and P2Y2 receptor agonist activities of uridine 5â²-phosphonate analogues
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and P2Y2 receptor agonist activities of uridine 5â²-phosphonate analogues Synthesis and P2Y2 receptor agonist activities of uridine 5â²-phosphonate analogues](/preview/png/10587182.png)
چکیده انگلیسی
We explored the influence of modifications of uridine 5â²-methylenephosphonate on biological activity at the human P2Y2 receptor. Key steps in the synthesis of a series of 5-substituted uridine 5â²-methylenephosphonates were the reaction of a suitably protected uridine 5â²-aldehyde with [(diethoxyphosphinyl)methylidene]triphenylphosphorane, C-5 bromination and a Suzuki-Miyaura coupling. These analogues behaved as selective agonists at the P2Y2 receptor, with three analogues exhibiting potencies in the submicromolar range. Although maximal activities observed with the phosphonate analogues were much less than observed with UTP, high concentrations of the phosphonates had no effect on the stimulatory effect of UTP. These results suggest that these phosphonates bind to an allosteric site of the P2Y2 receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 7, 1 April 2012, Pages 2304-2315
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 7, 1 April 2012, Pages 2304-2315
نویسندگان
Sara Van Poecke, Matthew O. Barrett, T. Santhosh Kumar, Davy Sinnaeve, José C. Martins, Kenneth A. Jacobson, T. Kendall Harden, Serge Van Calenbergh,