Design of BACE1 Inhibitors Containing 5-Nitro-IsophthaIamide

摘要

Previously, we reported non-peptidic BACE1 inhibitors possessing a hydroxymethylcarbonyl as a substrate transition-state mimic. In this study, we focused on isophthalamide structure as the P2 residue and designed KMI-1214 possessing 5-nitro-isophthalamide. Further SAR study led us to potent BACE1 inhibitors.