Synthesis and Evaluation of Benzimidazole Derivatives as Protein Tyrosine Phosphatase (PTP1B) Inhibitors

Type-II Diabetes is characterized by insulin resistance in various tissues along with defect in pancreatic cells. Protein tyrosine phosphatases (PTPs) selectively dephosphorylate the tyrosine residues and regulate various cellular processes. Protein tyrosine phosphatase 1B (PTP1B) emerged as a novel target for Type -II diabetes due to its negative regulatory effect on insulin signaling. Studies on PTP1B knockout mice confirms PTP1B as an effective target for drug discovery process for anti-diabetic and anti-obesity agents. In the present study Benzimidazole derivatives linked with various heterocyclic moieties were synthesized. The structure of the synthesized compounds were confirmed by IR, NMR and Mass spectroscopy. The compounds were evaluated for PTP1B enzyme inhibition using Calbiochem® colorimetric assay kit. Among all synthesized compounds 4f-4j had shown good PTP1B inhibitory, while other compounds have shown lesser potency as an anti-diabetic agent.