Synthesis and biological evaluation of some novel heterocyclic compounds as protein tyrosine phosphatase (PTP-1B) Inhibitor

Ashish Patel, T. Y. Pasha and

Abstract

Diabetes is a metabolic disorder wherein blood gluc ose level is increased along with some other abnorm al conditions like polyuria, polydipsia and polyphagia . As per WHO estimation, 380 million people will become diabetic by 2025. Tyrosine residues are selectively dephosphorylated by Protein tyrosine phosphatases (PTPs) and thus a wide variety of cellular processes are regul ated by their action. Protein tyrosine phosphatase 1B (PTP1 B) has shown to be a negative regulator in the insulin signaling pathways. Recent gene knockout studies c arried out on mice portrays PTP1B as an effective target for drug discovery process related to anti-diabetic and ant i-obese agents. PTPs are also involved in several other dis orders like cancer. The structure of compounds synt hesized by the present method were confirmed by TLC, IR, NMR a nd Mass spectroscopy. The anti-diabetic activity of the synthesized compounds were tested against PTP1B enz yme by using Calbiochem® PTP1B colorimetric assay k it. Among all synthesized compounds 4c, 4d, 4e, 4f had shown promising anti-diabetic activity, while o ther compounds have shown lesser potency as anti-diabetic agent

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