1215184-15-8Relevant articles and documents
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors
Aubele, Danielle L.,Truong, Anh P.,Dressen, Darren B.,Probst, Gary D.,Bowers, Simeon,Mattson, Matthew N.,Semko, Chris M.,Sun, Minghua,Garofalo, Albert W.,Konradi, Andrei W.,Sham, Hing L.,Zmolek, Wes,Wong, Karina,Goldbach, Erich,Quinn, Kevin P.,Sauer, John-Michael,Brigham, Elizabeth F.,Wallace, William,Nguyen, Lan,Bova, Michael P.,Hemphill, Susanna S.,Basi, Guriqbal
, p. 5791 - 5794 (2011/10/19)
The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate β-amyloid peptide synthesis via γ-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via a single PO dose, as well as sulfonamide-pyrazoles that exhibit selectivity for inhibition of APP versus Notch processing by γ-secretase, are highlighted.
