| Literature DB >> 18171614 |
Brian Clarke1, 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, Paul Rowland, Virginie Soleil, Kathrine J Smith, Steven Stanway, Geoffrey Stemp, Sharon Sweitzer, Pam Theobald, David Vesey, Daryl S Walter, John Ward, Gareth Wayne.
Abstract
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.Entities:
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Year: 2007 PMID： 18171614 DOI： 10.1016/j.bmcl.2007.12.017
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823