Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7- tetrahydropyridinoazole templates

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 21, 2012, Pages 6721-6727

  Sund, Christian ^a   Belda, Oscar ^a   Borkakoti, Neera ^a   Lindberg, Jimmy ^a   Derbyshire, Dean ^a   Vrang, Lotta ^a   Hamelink, Elizabeth ^a   Hgren, Cathrine ^a   Woestenenk, Esmeralda ^a   Wikström, Kristina ^a   Eneroth, Anders ^a   Lindström, Erik ^a   Kalayanov, Genadiy ^a  

^a MEDIVIR AB   (Sweden)

Author keywords

Secretase; A amyloid; Alzheimer's disease; BACE 1 inhibition; Hydroxylamine (HEA) isostere

Indexed keywords

4,5,6,7 TETRAHYDROBENZAZOLE; 4,5,6,7 TETRAHYDROPYRIDINOAZOLE; AMINE; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; BETA SITE AMYLOID PRECURSOR PROTEIN CLEAVING ENZYME 1 INHIBITOR; HYDROXYETHYLAMINE; PYRROLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CELL ASSAY; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYMATIC ASSAY; ENZYME INHIBITION; IC 50; MOLECULAR WEIGHT;

AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; AZOLES; BENZOXAZOLES; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME ACTIVATION; ENZYME INHIBITORS; ETHYLAMINES; HUMANS; INHIBITORY CONCENTRATION 50; MALE; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRIDINES;

EID: 84867571558     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.097     Document Type: Article

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