Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer’s disease

A novel series of 2-aminothiazoles with strong protection in an Alzheimer’s disease (AD) model comprising tau-induced neuronal toxicity is disclosed. These derivatives can be synthesized in one-pot and a small SAR of the substitution within these series afforded several compounds that counteracted tau-induced cell toxicity at nanomolar concentrations. These congeners therefore have strong potential as possible treatment for Alzheimer’s disease and other related tauopathies.

Graphical abstractSeveral derivatives with nanomolar inhibitory activity were uncovered with an IC50 of 14 nM for 3o as shown.Figure optionsDownload full-size imageDownload as PowerPoint slide