Thiazole-diamides as potent γ-secretase inhibitors

The thiazole-diamide series (1) has been identified as highly potent γ-secretase inhibitors. Several representative compounds showed IC50 values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [3H]-2a, are described.

The thiazole-diamide series has been identified as highly potent γ-secretase inhibitors. Several representative compounds showed IC50 values of <0.3 nM. The synthesis and SAR, as well as [3H]-2a, are described.Figure optionsDownload as PowerPoint slide