کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2481120 | 1556231 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer’s disease
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer’s disease Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer’s disease](/preview/png/2481120.png)
چکیده انگلیسی
A novel series of 2-aminothiazoles with strong protection in an Alzheimer’s disease (AD) model comprising tau-induced neuronal toxicity is disclosed. These derivatives can be synthesized in one-pot and a small SAR of the substitution within these series afforded several compounds that counteracted tau-induced cell toxicity at nanomolar concentrations. These congeners therefore have strong potential as possible treatment for Alzheimer’s disease and other related tauopathies.
Several derivatives with nanomolar inhibitory activity were uncovered with an IC50 of 14 nM for 3o as shown.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 43, Issue 5, 17 August 2011, Pages 386–392
Journal: European Journal of Pharmaceutical Sciences - Volume 43, Issue 5, 17 August 2011, Pages 386–392
نویسندگان
Irene Lagoja, Christophe Pannecouque, Gerard Griffioen, Stefaan Wera, Veronica Maria Rojasdelaparra, Arthur Van Aerschot,