Macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors with activity in vivo

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 5, 2009, Pages 1366-1370

  Machauer, Rainer ^a   Laumen, Kurt ^a   Veenstra, Siem ^a   Rondeau, Jean Michel ^a   Tintelnot Blomley, Marina ^a   Betschart, Claudia ^a   Jaton, Anne Lise ^a   Desrayaud, Sandrine ^a   Staufenbiel, Matthias ^a   Rabe, Sabine ^a   Paganetti, Paolo ^a   Neumann, Ulf ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Alzheimer's disease; BACE 1 inhibition; Ethanolamine transition state mimetic; In vivo efficacy in APP51 16 mice; Macrocycles

Indexed keywords

AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; AMYLOID PRECURSOR PROTEIN; BETA SECRETASE; BETA SECRETASE INHIBITOR; ETHANOLAMINE; MACROCYCLIC COMPOUND; NB 533; NB 544; UNCLASSIFIED DRUG; VALSPODAR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; C57BL 6 MOUSE; CELL ACTIVITY; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME ACTIVATION; ENZYME ACTIVITY; IN VIVO STUDY; MOUSE; NONHUMAN; TRANSGENIC MOUSE;

AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ENDOPEPTIDASES; CHO CELLS; CRICETINAE; CRICETULUS; CRYSTALLOGRAPHY, X-RAY; HUMANS; MACROCYCLIC COMPOUNDS; MICE; MICE, INBRED C57BL; MICE, TRANSGENIC; PEPTIDE FRAGMENTS; PROTEASE INHIBITORS; PROTEIN STRUCTURE, SECONDARY;

MUS; MUS MUSCULUS;

EID: 60449109719     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.055     Document Type: Article

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