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Molecules 2014, 19(1), 102-121; doi:10.3390/molecules19010102
Article

1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors

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Received: 31 October 2013 / Revised: 12 December 2013 / Accepted: 13 December 2013 / Published: 23 December 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Keywords: 1H-2,3-dihydroperimidine derivatives; PTP1B; inhibitors; selectivity; structure-activity relationships (SAR) 1H-2,3-dihydroperimidine derivatives; PTP1B; inhibitors; selectivity; structure-activity relationships (SAR)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Wang, W.-L.; Yang, D.-L.; Gao, L.-X.; Tang, C.-L.; Ma, W.-P.; Ye, H.-H.; Zhang, S.-Q.; Zhao, Y.-N.; Xu, H.-J.; Hu, Z.; Chen, X.; Fan, W.-H.; Chen, H.-J.; Li, J.-Y.; Nan, F.-J.; Li, J.; Feng, B. 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors. Molecules 2014, 19, 102-121.

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