- Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Bioorganic & medicinal chemistry letters (2013-01-15)
Xiaocong M Ye, 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
PMID23312944
RESUMEN
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.