Synthetic and Biological Studies of Some Pyrrolidine-Tethered Novel Aurones against Digestive Enzymes

Abstract

Abstract: Amylase, lipase, and trypsin are crucial digestive enzymes, whose activation or inhibition is of potent therapeutic approach for treating various body disorders. In this work, we have synthesized a small library of pyrrolidine-tethered novel aurones 4(a-k) and structures validated by analyzing their IR, NMR (1H and 13C), and mass spectrometry data. The biological activities of the synthesized aurones were evaluated through in vitro and in silico experiments against digestive enzymes. A distinct pattern emerged, with significant activation observed for trypsin and amylase, while lipase was notably inhibited. Among the synthesized compounds, 4f produced the highest lipase inhibition (72.3%), whereas 4k showed maximum activation for trypsin (EC50 = 0.94×10-6 M) and 4f activated amylase (EC50 = 8.76×10-4 M) to the maximum extent, thus confirming their possible use as agents for combating inflammation and obesity.