ABSTRACT
Diabetes mellitus (DM) is a heterogeneous group of disorders which is characterized by increased blood sugar level, altered metabolism of lipids, carbohydrates, and proteins and increased risk of complications from vascular disease. Protein Tyrosine Phosphatase 1B (PTP1B) has gained adequate notice due to its crucial role in type 2 diabetes (t2D) and obesity as a negative regulator of the insulin and leptin-signaling pathway. PTP-1B is primarily responsible for dephosphorylation of the insulin receptor and thus down regulates insulin signaling. PTP1B inhibitors are the latest candidate for the management of diabetes, where they prevent dephosphorylation of the insulin receptor and consequently increase insulin level. Natural products have been reported to exhibit promising anti-diabetic activity. Chalcones or 1,3-diphenyl-2E-propene-1-one, the open chain intermediate in aurones synthesis of flavones containing benzylideneacetophenone scaffold, where the two aromatic nuclei are joined by a three-carbon α, β 236unsaturated carbonyl bridge have shown tremendous PTP1B inhibition. In this chapter, a concrete focus on pharmacology, mechanism of action, and structural aspects along with substituents required for modulating PTP1B has been discussed. Still, none of these inhibitors have gained adequate attention at present and need to be explored and evaluated properly in terms of efficacy and toxicity to develop as therapeutic agents/formulations for the management of diabetes in future.
