کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371878 | 981857 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer’s disease
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Utilizing structure-based drug design, a 4-aminoimidazole heterocyclic core was synthesized as a replacement for a 2-aminothiazole due to potential metabolically mediated toxicity. The synthetic route utilized allowed for ready synthesis of 1-substituted-4-aminoimidazoles. SAR exploration resulted in the identification of a novel cis-substituted cyclobutyl group that gave improved enzyme and cellular potency against cdk5/p25 with up to 30-fold selectivity over cdk2/cyclin E.
Using structure-based drug design, 4-aminoimidazoles were prepared with potent inhibition of cdk5/p25 in enzyme and whole cell assays and selectivity over cdk2.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5703–5707
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5703–5707
نویسندگان
Christopher J. Helal, Zhijun Kang, John C. Lucas, Thomas Gant, Michael K. Ahlijanian, Joel B. Schachter, Karl E.G. Richter, James M. Cook, Frank S. Menniti, Kristin Kelly, Scot Mente, Jay Pandit, Natalie Hosea,