BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells

Modifications to the non-prime side of a series of BACE-1 inhibitors are presented. This final round of optimisation led to inhibitors with nanomolar potency in a cell-based assay which were capable of lowering amyloid production in an animal model following oral administration. This article is focu...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-02, Vol.18 (3), p.1022-1026
Hauptverfasser: Beswick, Paul, Charrier, Nicolas, Clarke, Brian, Demont, Emmanuel, Dingwall, Colin, Dunsdon, Rachel, Faller, Andrew, Gleave, Robert, Hawkins, Julie, Hussain, Ishrut, Johnson, Christopher N., MacPherson, David, Maile, Graham, Matico, Rosalie, Milner, Peter, Mosley, Julie, Naylor, Alan, O’Brien, Alistair, Redshaw, Sally, Riddell, David, Rowland, Paul, Skidmore, John, Soleil, Virginie, Smith, Kathrine J., Stanway, Steven, Stemp, Geoffrey, Stuart, Alistair, Sweitzer, Sharon, Theobald, Pam, Vesey, David, Walter, Daryl S., Ward, John, Wayne, Gareth
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Sprache:eng
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