2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039.
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

Affiliation

  • 1 Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd., South San Francisco, CA 94080, USA. mxcye@hotmail.com
PMID: 23312944 DOI: 10.1016/j.bmcl.2012.12.039
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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