Synthesis And Biological Activity Studies Of Derivatives Of Chalcone In Diabetes Mellitus

Natural chalcone has a wide range of pharmacological activity,such as anti-tumor,anti-bacterial,anti-inflammatory.We designed 48 compounds according to the structure of chalcone.Through molecular docking with PTP1 B,we screened out 17 compounds exhibited inhibitory activity against PTP1 B.In this paper,we designed the synthetic routes of the target compounds,and successfully synthesized 11 compounds from 2-hydroxyacetophenone and 2,4,6-trihydroxyacetophenone.The structures of the target compounds were characterized by nuclear magnetic resonance spectroscopy,carbon spectroscopy and high resolution mass spectrometry.In vitro activity data show that most compounds had significant inhibitory effect on PTP1 B at 16.7?g/ml.Structure-activity relationship studies have shown that the number of hydroxyl groups has a significant effect on the activity of the compounds and chalcone compound d11 has the strongest inhibitory activity against PTP1 B.