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. 2013 Feb 15;23(4):996-1000.
doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21.

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

Xiaocong M Ye  1 , Andrei W Konradi, Minghua Sun, Shendong Yuan, Danielle L Aubele, Michael Dappen, Darren Dressen, Albert W Garofalo, Jacek J Jagodzinski, Lee Latimer, Gary D Probst, Hing L Sham, David Wone, Ying-zi Xu, Daniel Ness, Elizabeth Brigham, Grace T Kwong, Chris Willtis, George Tonn, Erich Goldbach, Kevin P Quinn, Hongbin H Zhang, John-Michael Sauer, Michael Bova, Guriqbal S Basi
Affiliations

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

Xiaocong M Ye et al. Bioorg Med Chem Lett. .

Abstract

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.

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