Discovery of Ursolic Acid Derivatives as Inhibitors of Protein Tyrosine Phosphatase 1B

Here, a series of ursolic acid (UA) derivatives were identified as potential protein tyrosine phosphatase 1B (PTP1B) enzyme inhibitors. All of the tested compounds showed potent PTP1B inhibitory activity (47.01–67.89%). Compound 2d (67.89%) exhibited the highest activity of all the synthesized compounds, which showed higher activity than observed for the positive control UA (51.13%). Molecular docking simulation and analysis suggested that compound 2d has a good binding interaction with the active pocket.