کد مقاله کد نشریه سال انتشار مقاله انگلیسی ترجمه فارسی نسخه تمام متن
1360686 981443 2017 13 صفحه PDF ندارد دانلود رایگان
عنوان انگلیسی مقاله
Design, synthesis and structure–activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β
ترجمه فارسی عنوان
طراحی، سنتز و روابط ساختار فعالیت مشتقات 1،3،4-oxadiazole به عنوان مهار کننده جدیدی گلیکوژن سنتاز کیناز 3β
کلمات کلیدی
GSK-3β؛ بیماری آلزایمر؛ Oxadiazole؛ طراحی دارو
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Glycogen synthase kinase-3β (GSK-3β) is implicated in abnormal hyperphosphorylation of tau protein and its inhibitors are expected to be a promising therapeutic agents for the treatment of Alzheimer’s disease. Here we report design, synthesis and structure–activity relationships of a novel series of oxadiazole derivatives as GSK-3β inhibitors. Among these inhibitors, compound 20x showed highly selective and potent GSK-3β inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GSK-3β.

Graphical abstractDesign, synthesis and structure–activity relationships of novel oxadiazole derivatives as GSK-3β inhibitors are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 5, 1 March 2009, Pages 2017–2029
نویسندگان
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