کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377333 | 981976 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer’s disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of potent inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic. These inhibitors were capable of lowering amyloid production in a cell-based assay.
The discovery of novel BACE-1 inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic is described: X-ray crystallography facilitated the rapid optimisation of a micromolar hit and led to inhibitors capable of lowering amyloid production in a cell-based assay.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 3, 1 February 2008, Pages 1011–1016
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 3, 1 February 2008, Pages 1011–1016
نویسندگان
Brian Clarke, Emmanuel Demont, Colin Dingwall, Rachel Dunsdon, Andrew Faller, Julie Hawkins, Ishrut Hussain, David MacPherson, Graham Maile, Rosalie Matico, Peter Milner, Julie Mosley, Alan Naylor, Alistair O’Brien, Sally Redshaw, David Riddell,