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Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 19, 2013, Pages 5300-5306

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: Structure based design and in vivo reduction of amyloid β-peptides

(10) Rueeger, Heinrich a Lueoend, Rainer a Machauer, Rainer a Veenstra, Siem Jacob a Jacobson, Laura Helen a,b Staufenbiel, Matthias a Desrayaud, Sandrine a Rondeau, Jean Michel a Möbitz, Henrik a Neumann, Ulf a

a NOVARTIS PHARMA AG (Switzerland)

b UNIVERSITY OF MELBOURNE (Australia)

Author keywords

peptides; Alzheimer's disease; BACE 1; Cyclic sulfoxide hydroxyethylamine inhibitors; In vivo reduction of amyloid; Inhibitor; Structure based design

Indexed keywords

AMINE; AMYLOID BETA PROTEIN; ASPARTIC PROTEINASE INHIBITOR; BETA SECRETASE 1; RITONAVIR; SULFOXIDE;

ANIMAL EXPERIMENT; ARTICLE; COLUMN CHROMATOGRAPHY; CONTROLLED STUDY; DRUG CLEARANCE; FEMALE; IC 50; MALE; MOUSE; NONHUMAN; REDUCTION; STRUCTURE ACTIVITY RELATION;

MUS;

ALZHEIMER'S DISEASE; BACE-1; CYCLIC SULFOXIDE HYDROXYETHYLAMINE INHIBITORS; IN VIVO REDUCTION OF AMYLOID Β-PEPTIDES; INHIBITOR; STRUCTURE BASED DESIGN;

AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BRAIN CHEMISTRY; CRYSTALLOGRAPHY, X-RAY; CYCLIZATION; DRUG DISCOVERY; ENZYME ACTIVATION; ENZYME INHIBITORS; ETHANOLAMINES; FEMALE; INHIBITORY CONCENTRATION 50; MALE; MICE; MOLECULAR STRUCTURE; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; SULFOXIDES;

EID: 84883488261 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2013.07.071 Document Type: Article

Times cited : (24)

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