Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 4, 2013, Pages 996-1000

  Ye, Xiaocong M ^a   Konradi, Andrei W ^a   Sun, Minghua ^a   Yuan, Shendong ^a   Aubele, Danielle L ^a   Dappen, Michael ^a   Dressen, Darren ^a   Garofalo, Albert W ^a   Jagodzinski, Jacek J ^a   Latimer, Lee ^a   Probst, Gary D ^a   Sham, Hing L ^a   Wone, David ^a   Xu, Ying Zi ^a   Ness, Daniel ^a   Brigham, Elizabeth ^a   Kwong, Grace T ^a   Willtis, Chris ^a   Tonn, George ^a   Goldbach, Erich ^a   Quinn, Kevin P ^a   Zhang, Hongbin H ^a   Sauer, John Michael ^a   Bova, Michael ^a   Basi, Guriqbal S ^a   more..

^a ELAN PHARMACEUTICALS   (United States)

Author keywords

Secretase; Secretase inhibitor; Alzheimer's disease; Amyloid precursor protein; Notch

Indexed keywords

AMYLOID BETA PROTEIN[1-40]; AMYLOID PRECURSOR PROTEIN; AVAGACESTAT; BEGACESTAT; ELND 006; FUNCTIONAL GROUP; GAMMA SECRETASE INHIBITOR; PYRAZOLE DERIVATIVE; SULFONAMIDE; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BRAIN CORTEX; BRAIN LEVEL; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG METABOLISM; DRUG POTENCY; DRUG SELECTIVITY; ENANTIOMER; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; IC 50; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; RAT; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; BICYCLO COMPOUNDS, HETEROCYCLIC; MICE; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

MUS;

EID: 84872928749     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.12.039     Document Type: Article

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