| Literature DB >> 18171615 |
Paul Beswick1, Nicolas Charrier, Brian Clarke, Emmanuel Demont, Colin Dingwall, Rachel Dunsdon, Andrew Faller, Robert Gleave, Julie Hawkins, Ishrut Hussain, Christopher N Johnson, David MacPherson, Graham Maile, Rosalie Matico, Peter Milner, Julie Mosley, Alan Naylor, Alistair O'Brien, Sally Redshaw, David Riddell, Paul Rowland, John Skidmore, Virginie Soleil, Kathrine J Smith, Steven Stanway, Geoffrey Stemp, Alistair Stuart, Sharon Sweitzer, Pam Theobald, David Vesey, Daryl S Walter, John Ward, Gareth Wayne.
Abstract
This article is focusing on further optimization of previously described hydroxy ethylamine (HEA) BACE-1 inhibitors obtained from a focused library with the support of X-ray crystallography. Optimization of the non-prime side of our inhibitors and introduction of a 6-membered sultam substituent binding to Asn-294 as well as a fluorine in the C-2 position led to derivatives with nanomolar potency in cell-based assays.Entities:
Mesh：
Substances：
Year: 2007 PMID： 18171615 DOI： 10.1016/j.bmcl.2007.12.020
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823