SYNTHESIS AND ACTIVITY OF BENZO-CHALCONE DERIVATIVES AS PTP1B INHIBITORS
Protein tyrosine phosphodiesterase 1B(PTP1B),a member of the non-receptor PTPase family,is involved in the regulation of many physiological and pathological processes,especially the regulation of energy and glucose homeostasis in the insulin signaling pathway.It has been identified as a potential therapeutic target for the treatment of diabetes and obesity.In this study,a series of hydroxy-contained benzo-chalcones and their cyclic derivatives(1a-1g,2a-2g)were designed and synthesized using computer-based drug design methodology based on the PTP1B active site.And their inhibitory activity against PTP1B enzyme was evaluated.In the present study,four active PTP1B inhibitors were obtained with IC50 values of 1.91,8.59,7.38,and 4.64 μM,respectively.This study provides a new direction for the development of novel PTP1B inhibitors with good cell permeability and bioavailability.
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