Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as γ-secretase inhibitors are described. Compounds that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via oral dose, as well as those with high selectivity over Notch, are highlighted.
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.
p. 996 - 1000
(2013/03/13)
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