Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent [gamma]-secretase inhibitors
The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate [beta]-amyloid peptide synthesis via [gamma]-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficacious in reducing the cortical A[beta]x-40 l...
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Published in | Bioorganic & medicinal chemistry letters Vol. 21; no. 19; pp. 5791 - 5794 |
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Main Authors | , , , , , , , , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
01.10.2011
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Online Access | Get full text |
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Summary: | The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate [beta]-amyloid peptide synthesis via [gamma]-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficacious in reducing the cortical A[beta]x-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 [gamma]-secretase, are highlighted. |
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Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 content type line 23 ObjectType-Feature-1 |
ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2011.08.008 |