Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 1, 2008, Pages 418-422

  Iserloh, U ^a   Pan, J ^a   Stamford, A W ^a   Kennedy, M E ^a   Zhang, Q ^a   Zhang, L ^a   Parker, E M ^a   McHugh, N A ^a   Favreau, L ^a   Strickland, C ^a   Voigt, J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Secretase inhibitors; Alzheimer's disease; Aspartyl proteases

Indexed keywords

4 PHENOXYPYRROLIDINE DERIVATIVE; AMIDE; AMINE; AMYLOID BETA PROTEIN[1-40]; BETA AMYLOID CONVERTING ENZYME 1; BETA AMYLOID CONVERTING ENZYME 1 INHIBITOR; BETA AMYLOID CONVERTING ENZYME 2; BETA SECRETASE INHIBITOR; CATHEPSIN D; CATHEPSIN E; PEPSIN A; PYRROLIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG SCREENING; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; AMIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ENDOPEPTIDASES; CRYSTALLOGRAPHY, X-RAY; HUMANS; HYDROGEN BONDING; MICE; MICE, TRANSGENIC; MODELS, MOLECULAR; PHENOLS; PROTEASE INHIBITORS; PYRROLIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 37549069915     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.10.053     Document Type: Article

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