Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor

Journal of Medicinal Chemistry

Volumn 55, Issue 7, 2012, Pages 3414-3424

  Stepan, Antonia F ^a   Subramanyam, Chakrapani ^a   Efremov, Ivan V ^a   Dutra, Jason K ^a   O'Sullivan, Theresa J ^a   Dirico, Kenneth J ^a   McDonald, W Scott ^a   Won, Annie ^a   Dorff, Peter H ^a   Nolan, Charles E ^a   Becker, Stacey L ^a   Pustilnik, Leslie R ^a   Riddell, David R ^a   Kauffman, Gregory W ^a   Kormos, Bethany L ^a   Zhang, Liming ^a   Lu, Yasong ^a   Capetta, Steven H ^a   Green, Michael E ^a   Karki, Kapil ^a   Sibley, Evelyn ^a   Atchison, Kevin P ^a   Hallgren, Andrew J ^a   Oborski, Christine E ^a   Robshaw, Ashley E ^a   Sneed, Blossom ^a   O'Donnell, Christopher J ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [N [[3 (1,2,4 OXADIAZOL 3 YL)BICYCLO[1.1.1]PENTAN 1 YL] METHYL] 4 CHLOROPHENYLSULFONAMIDO] 5,5,5 TRIFLUOROPENTANAMIDE; AVAGACESTAT; CYCLOPENTANE DERIVATIVE; GAMMA SECRETASE INHIBITOR; PHENYL GROUP; UNCLASSIFIED DRUG; WATER;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG DESIGN; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; RAT; SINGLE DRUG DOSE;

EID: 84859797196     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300094u     Document Type: Article

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