Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious [gamma]-secretase inhibitors

Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as [gamma]-secretase inhibitors are described. Compounds that are efficacious in reducing the cortical A[beta]x-40 levels in FVB mice via oral dose, as well as tho...

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Published inBioorganic & medicinal chemistry letters Vol. 23; no. 4; pp. 996 - 1000
Main Authors Ye, Xiaocong M, Konradi, Andrei W, Sun, Minghua, Yuan, Shendong, Aubele, Danielle L, Dappen, Michael, Dressen, Darren, Garofalo, Albert W, Jagodzinski, Jacek J, Latimer, Lee, Probst, Gary D, Sham, Hing L, Wone, David, Xu, Ying-zi, Ness, Daniel, Brigham, Elizabeth, Kwong, Grace T, Willtis, Chris, Tonn, George, Goldbach, Erich, Quinn, Kevin P, Zhang, Hongbin H, Sauer, John-Michael, Bova, Michael, Basi, Guriqbal S
Format Journal Article
LanguageEnglish
Published 15.02.2013
Subjects
Cortex
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Summary:Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as [gamma]-secretase inhibitors are described. Compounds that are efficacious in reducing the cortical A[beta]x-40 levels in FVB mice via oral dose, as well as those with high selectivity over Notch, are highlighted.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
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ISSN:0960-894X