Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372545 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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.
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Authors
Danielle L. Aubele, Anh P. Truong, Darren B. Dressen, Gary D. Probst, Simeon Bowers, Matthew N. Mattson, Chris M. Semko, Minghua Sun, Albert W. Garofalo, Andrei W. Konradi, Hing L. Sham, Wes Zmolek, Karina Wong, Erich Goldbach, Kevin P. Quinn,