Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors

Journal of Medicinal Chemistry

Volumn 54, Issue 22, 2011, Pages 7772-7783

  Stepan, Antonia F ^a   Karki, Kapil ^a   McDonald, W Scott ^a   Dorff, Peter H ^a   Dutra, Jason K ^a   Dirico, Kenneth J ^a   Won, Annie ^a   Subramanyam, Chakrapani ^a   Efremov, Ivan V ^a   O'Donnell, Christopher J ^a   Nolan, Charles E ^a   Becker, Stacey L ^a   Pustilnik, Leslie R ^a   Sneed, Blossom ^a   Sun, Hao ^a   Lu, Yasong ^a   Robshaw, Ashley E ^a   Riddell, David ^a   O'Sullivan, Theresa J ^a   Sibley, Evelyn ^a   Capetta, Steven ^a   Atchison, Kevin ^a   Hallgren, Andrew J ^a   Miller, Emily ^a   Wood, Anthony ^a   Obach, R Scott ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 CHLORO N (CYCLOBUTYLMETHYL)PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N (CYCLOHEXYLMETHYL)PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N (CYCLOPENTYLMETHYL)PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N (OXETAN 2 YLMETHYL) PHENYLSULFONAMIDO]5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N (OXETAN 2 YLMETHYL)PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N (OXETAN 3 YLMETHYL)PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [4 CHLORO N [(TETRAHYDRO 2H PYRAN 2 YL)METHYL] PHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; 2 [N [(1,4 DIOXAN 2 YL)METHYL] 4 CHLOROPHENYLSULFONAMIDO] 5,5,5 TRIFLUORPENTANAMIDE; AVAGACESTAT; BEGACESTAT; BMS 299897; CYTOCHROME P450 3A4; GAMMA SECRETASE INHIBITOR; OXETANE DERIVATIVE; PF 3084014; SEMAGACESTAT; SULFONAMIDE; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; DRUG DESIGN; DRUG STRUCTURE; ENZYME ACTIVE SITE; HUMAN; HUMAN CELL; IN VIVO STUDY; ISOMER; LIPOPHILICITY; LIVER MICROSOME; MALE; METABOLISM; MOUSE; NONHUMAN; OXIDATION; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; BRAIN; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DOGS; DRUG DESIGN; ETHERS, CYCLIC; HUMANS; MICE; MICROSOMES, LIVER; OXIDATION-REDUCTION; RECEPTORS, NOTCH; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TISSUE DISTRIBUTION;

EID: 81555223843     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200893p     Document Type: Article

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