Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer’s disease

Abstract Herein we describe the structure–activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1 , highlighting affects on the potency of γ-secretase inhibition, selectivity for the inhibition of APP versus Notch processing by γ-secretase and selected pharmakokinetic properties. Amino-caprolactams that are efficacious in reducing the cortical Aβ x-40 levels in FVB mice via a single 100 mpk IP dose are highlighted.