4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors

We have designed and synthesized a novel series of 3-biphenylamino acid amides as cathepsin K inhibitors based on compound I. In these inhibitors, we have discovered 4-aminophenoxyacetic acids 43 and 47 with good IC50 values, although lipophilic groups are favorable for the hydrophobic S1′ pocket.

Graphical abstractThe synthesis and SAR of 4-aminophenoxyacetic acids as cathepsin K inhibitors are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide