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

Article abstract of DOI:10.1016/j.bmc.2009.04.052

γ-Secretase inhibitors have been shown to reduce the production of β-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide γ-secretase inhibitors that reduce β-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 γ-secretase substrate.