| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370825 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
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 Aβx-40 levels in FVB mice via a single 100 mpk IP dose are highlighted.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Martin L. Neitzel, Danielle L. Aubele, Jennifer L. Marugg, Jacek J. Jagodzinski, Andrei W. Konradi, Michael A. Pleiss, Balazs Szoke, Wes Zmolek, Erich Goldbach, Kevin P. Quinn, John-Michael Sauer, Elizabeth F. Brigham, William Wallace, Michael P. Bova,