1215181-92-2Relevant articles and documents
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
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)
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.