BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 3, 2008, Pages 1011-1016

  Clarke, Brian ^a   Demont, Emmanuel ^a   Dingwall, Colin ^a   Dunsdon, Rachel ^a   Faller, Andrew ^a   Hawkins, Julie ^a   Hussain, Ishrut ^a   MacPherson, David ^a   Maile, Graham ^a   Matico, Rosalie ^a   Milner, Peter ^a   Mosley, Julie ^a   Naylor, Alan ^a   O'Brien, Alistair ^a   Redshaw, Sally ^a   Riddell, David ^a   Rowland, Paul ^a   Soleil, Virginie ^a   Smith, Kathrine J ^a   Stanway, Steven ^a   Stemp, Geoffrey ^a   Sweitzer, Sharon ^a   Theobald, Pam ^a   Vesey, David ^a   Walter, Daryl S ^a   Ward, John ^a   Wayne, Gareth ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Alzheimer; Aspartic protease; BACE 1; Hydroxy ethylamine

Indexed keywords

AMYLOID; BETA SECRETASE INHIBITOR; ETHYLAMINE;

ARTICLE; CELL ASSAY; CRYSTAL STRUCTURE; DRUG IDENTIFICATION; DRUG STRUCTURE; ENZYME INHIBITION; MOLECULAR MIMICRY; X RAY CRYSTALLOGRAPHY;

ALZHEIMER DISEASE; AMYLOID BETA-PROTEIN PRECURSOR; ASPARTIC ENDOPEPTIDASES; COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; ETHYLAMINES; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 38749086822     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.12.017     Document Type: Article

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21. Substitution ortho to the amide functionality was in general poorly tolerated (data not shown).
22. free = 0.227).
23. This effect was also observed with HBAs other than pyrrolidinone.