Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (bace1) inhibitors

Journal of Medicinal Chemistry

Volumn 57, Issue 23, 2014, Pages 9796-9810

  Epstein, Oleg ^a,b   Bryan, Marian C ^a,b,c   Cheng, Alan C ^a,b   Derakhchan, Katayoun ^a,b   Dineen, Thomas A ^a,b   Hickman, Dean ^a,b   Hua, Zihao ^a,b   Human, Jason B ^a,b   Kreiman, Charles ^a,b   Marx, Isaac E ^a,b   Weiss, Matthew M ^a,b   Wahl, Robert C ^a,b   Wen, Paul H ^a,b   Whittington, Douglas A ^a,b   Wood, Stephen ^a,b   Zheng, Xiao Mei ^a,b   Fremeau, Robert T ^a,b   White, Ryan D ^a,b   Patel, Vinod F ^a,b,d  

^a AMGEN INC   (United States)

^b Neuroscience Amgen Inc ^*  (United States)

^c GENENTECH INC   (United States)

^d Sanofi   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINOOXAZOLINE XANTHENE; BETA SECRETASE 1; ION CHANNEL; NOOTROPIC AGENT; ORGANOTIN COMPOUND; PALLADIUM; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG; XANTHENE; XANTHENE DERIVATIVE; ASPARTIC PROTEINASE; BACE1 PROTEIN, HUMAN; OXAZOLONE; PROTEINASE INHIBITOR; SECRETASE;

ALKYLATION; ALZHEIMER DISEASE; ARTICLE; BINDING ASSAY; DEMETHYLATION; ENZYME ACTIVITY; IC50; IN VITRO STUDY; PROCESS OPTIMIZATION; SONOGASHIRA REACTION; SUZUKI REACTION; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; HEK293 CELL LINE; HUMAN; LIVER MICROSOME; MALE; METABOLISM; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; CRYSTALLOGRAPHY, X-RAY; ETHER-A-GO-GO POTASSIUM CHANNELS; HEK293 CELLS; HUMANS; INHIBITORY CONCENTRATION 50; MALE; MICROSOMES, LIVER; OXAZOLONE; PROTEASE INHIBITORS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP; XANTHENES;

EID: 84918589185     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501266w     Document Type: Article

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