Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 11, 2012, Pages 3607-3611

  Monenschein, Holger ^b   Horne, Daniel B ^a   Bartberger, Michael D ^a   Hitchcock, Stephen A ^b   Nguyen, Thomas T ^a   Patel, Vinod F ^c   Pennington, Lewis D ^a   Zhong, Wenge ^a  

^a AMGEN INC   (United States)

^b Envoy Therapeutics   (United States)

^c Sanofi Aventis   (United States)

Author keywords

secretase; A amyloid; Alzheimer's disease; Aspartyl protease; BACE inhibitors; Hydroxyethylene derivatives; Protease inhibitors

Indexed keywords

1 ETHOXYCYCLOPROPOXY TRIMETHYLSILANE; 2 HYDROXYL CHROMANS; 2 METHYLCYCLOBUTANONE; 2 METHYLPROPANE 1,3 DIOL; 3 HYDROXY CHROMAN; 3 HYDROXYCYCLOBUTANE; 3 METHYLCYCLOBUTANONE; 3,3 DIFLUORO CYCLOBUTANE; 8 AZACHROMAN AMINE; ALLYLCYCLOBUTANE; BETA SECRETASE; BETA SECRETASE INHIBITOR; CATHEPSIN D; CHROMAN DERIVATIVE; CYCLOBUTANONE DERIVATIVE; DITHIANE; SPIROCYCLOBUTYL COMPOUND; SULFINIMINE; UNCLASSIFIED DRUG; VINYL CYCLOPROPANE; VINYL PIVALATE;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; DRUG ACTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN TISSUE; NONHUMAN; RAT;

ALZHEIMER DISEASE; AMYLOID PRECURSOR PROTEIN SECRETASES; BINDING SITES; CATALYTIC DOMAIN; CATHEPSIN D; COMPUTER SIMULATION; ETHYLAMINES; HUMANS; MICROSOMES, LIVER; PROTEASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84861196665     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.04.060     Document Type: Article

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