Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structure–activity relationships?

MedChemComm Pub Date: 2013-08-19 DOI: 10.1039/C3MD00138E

Abstract

The protein tyrosine phosphatase 1B (PTP1B) is an attractive target for the treatment of type 2 diabetes. A series of substituted 1,3-benzyl urea has been synthesized and evaluated for PTP1B inhibitory, antidiabetic and antidyslipidemic activities. The most active compound of the series 5b showed 79.4% PTP1B inhibition and 20.7% blood glucose lowering in the STZ model. It also lowered the serum cholesterol level by 16.3% and significantly increased the serum HDL-cholesterol by 46.8%. The high activity of compound 5b has been explained by docking studies.

Graphical abstract: Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structure–activity relationships
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