Discovery of a series of efficient, centrally efficacious bace1 inhibitors through structure-based drug design

Journal of Medicinal Chemistry

Volumn 58, Issue 6, 2015, Pages 2678-2702

  Butler, Christopher R ^a   Brodney, Michael A ^a   Beck, Elizabeth M ^a   Barreiro, Gabriela ^b   Nolan, Charles E ^a   Pan, Feng ^a   Vajdos, Felix ^a   Parris, Kevin ^a   Varghese, Alison H ^a   Helal, Christopher J ^a   Lira, Ricardo ^a   Doran, Shawn D ^a   Riddell, David R ^a   Buzon, Leanne M ^a   Dutra, Jason K ^a   Martinez Alsina, Luis A ^a   Ogilvie, Kevin ^a   Murray, John C ^a   Young, Joseph M ^a   Atchison, Kevin ^a   Robshaw, Ashley ^a   Gonzales, Cathleen ^a   Wang, Jinlong ^c   Zhang, Yong ^c   Oneill, Brian T ^a   more..

^a PFIZER INC   (United States)

^b Departamento de Inovacao Eurofarma Laboratorios SA   (Brazil)

^c WUXI APPTEC   (China)

Author keywords

[No Author keywords available]

Indexed keywords

8A (2,4 DIFLUOROPHENYL) 6 (FLUOROMETHYL) 4,4A,5,6,8,81 HEXAHYDROPYRANO[3,4 D][1,3]THIAZIN 2 AMINE; AMYLOID BETA PROTEIN; BETA SECRETASE 1; BETA SECRETASE 1 INHIBITOR; BETA SECRETASE INHIBITOR; CATHEPSIN D; THIOAMIDE; UNCLASSIFIED DRUG; AMIDINE; ASPARTIC PROTEINASE; BACE1 PROTEIN, HUMAN; ENZYME INHIBITOR; SECRETASE; THIOL DERIVATIVE;

ALZHEIMER DISEASE; AMYLOID PLAQUE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTOFLUORESCENCE; BEAGLE; CHRONIC DRUG ADMINISTRATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG EFFICACY; DRUG SCREENING; DRUG SELECTIVITY; HISTOLOGY; MALE; MOUSE; NONHUMAN; PIGMENT EPITHELIUM; STRUCTURE ACTIVITY RELATION; TOXICITY TESTING; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; CHEMICAL STRUCTURE; CHEMISTRY; DOG; DRUG EFFECTS; HUMAN; METABOLISM; PATHOLOGY; PLAQUE, AMYLOID; RAT; WISTAR RAT;

ALZHEIMER DISEASE; AMIDINES; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BRAIN; DOGS; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; MALE; MICE; MODELS, MOLECULAR; PLAQUE, AMYLOID; RATS; RATS, WISTAR; SULFHYDRYL COMPOUNDS;

EID: 84925957189     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501833t     Document Type: Article

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