Abstract
In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake using L6 muscle cell lines and enzymatic assay against PTP1B. The biological activity results showed that the 2-methoxy substituted (14b) compound exhibited significant activity in both the assays. The unsubstituted compound (14a) also possessed comparable activity on glucose reuptake in L6 muscle cell lines and better inhibitory activity on PTP1B enzyme assays. Docking analysis was performed on the most potent compound of the series to understand the nature of interactions governing the binding of the designed molecule with the PTP1B enzyme.
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Acknowledgments
The authors gratefully acknowledge SAIF, Punjab University, Chandigarh for NMR spectral analysis of the synthesized compounds. The author Girdhar Singh Deora wishes to thank AICTE, New Delhi for postgraduate fellowship. C. Karthikeyan is a recipient of a senior research fellowship of CSIR, New Delhi.
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Deora, G.S., Karthikeyan, C., Moorthy, N.S.H.N. et al. Design, synthesis and biological evaluation of novel arylidine-malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B. Med Chem Res 22, 5344–5348 (2013). https://doi.org/10.1007/s00044-013-0528-1
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DOI: https://doi.org/10.1007/s00044-013-0528-1