Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of alzheimers disease: Utilization of structure based drug design, watermap, and cns penetration studies to identify centrally efficacious inhibitors

Journal of Medicinal Chemistry

Volumn 55, Issue 21, 2012, Pages 9224-9239

  Brodney, Michael A ^a   Barreiro, Gabriela ^a   Ogilvie, Kevin ^a   Hajos Korcsok, Eva ^a   Murray, John ^a   Vajdos, Felix ^a   Ambroise, Claude ^a   Christoffersen, Curt ^a   Fisher, Katherine ^a   Lanyon, Lorraine ^a   Liu, Jianhua ^a   Nolan, Charles E ^a   Withka, Jane M ^a   Borzilleri, Kris A ^a   Efremov, Ivan ^a   Oborski, Christine E ^a   Varghese, Alison ^a   Oneill, Brian T ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[[1 (3 FLUOROPHENYL) 3,7 DIMETHYL 2,2 DIOXIDO 2 THIA 1,3,8 TRIAZASPIRO[4.5]DEC 8 YL]METHYL] 2 ISOPROPOXYPHENOL; AMYLOID BETA PROTEIN; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; MULTIDRUG RESISTANCE PROTEIN; SPIRO COMPOUND; SULFAMIDE DERIVATIVE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CENTRAL NERVOUS SYSTEM; COMPUTER MODEL; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG EFFICACY; DRUG EXPOSURE; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; ENZYME INHIBITION; FEMALE; HYDROGEN BOND; IC 50; MEMBRANE PERMEABILITY; MEMBRANE TRANSPORT; MOUSE; NONHUMAN; PROTEIN TRANSPORT; STRUCTURE ACTIVITY RELATION;

ALZHEIMER DISEASE; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; AZA COMPOUNDS; BRAIN; CRYSTALLOGRAPHY, X-RAY; DOGS; DRUG DESIGN; FEMALE; HUMANS; MADIN DARBY CANINE KIDNEY CELLS; MALE; MICE; MICE, KNOCKOUT; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; P-GLYCOPROTEIN; PERMEABILITY; SPIRO COMPOUNDS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TRANSFECTION;

EID: 84868550667     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3009426     Document Type: Article

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