Potent transglutaminase inhibitors, aryl β-aminoethyl ketones

Aryl β-aminoethyl ketones were discovered as potent inhibitors of tissue transglutaminase. Heteroaryl-like thiophene groups and N-benzyl N-t-butyl aminoethyl group are critical to the strong inhibitory activity of aryl β-aminoethyl ketones.

We report on potent inhibitors of tissue transglutaminase implicated in various diseases ranging from celiac disease and neurodegenerative disorders such as Alzheimer’s, Huntington’s, and Parkinson’s diseases.Figure optionsDownload as PowerPoint slide