2. Academic Validation
  3. Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors

Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors

  • Bioorg Med Chem. 2009 Jul 1;17(13):4708-17. doi: 10.1016/j.bmc.2009.04.052.
Jun Pu 1,  Anthony F Kreft,  Suzan H Aschmies,  Kevin P Atchison,  Joshua Berkowitz,  Thomas J Caggiano,  Micheal Chlenov,  George Diamantidis,  Boyd L Harrison,  Yun Hu,  Donna Huryn,  J Steven Jacobsen,  Mei Jin,  Kerri Lipinski,  Peimin Lu,  Robert L Martone,  Koi Morris,  June Sonnenberg-Reines,  Dave R Riddell,  Joan Sabalski,  Shaiu-Ching Sun,  Erik Wagner,  Yiqun Wang,  Zheng Xu,  Hua Zhou,  Lynn Resnick
Affiliations

Affiliation

  • 1 Chemical Sciences, Wyeth Research, Princeton, NJ 08543-8000, USA.
PMID: 19443228 DOI: 10.1016/j.bmc.2009.04.052
Abstract

gamma-Secretase inhibitors have been shown to reduce the production of beta-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide gamma-secretase inhibitors that reduce beta-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative gamma-secretase substrate.

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