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

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

1
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China
2
State key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
3
Jiangshu Alpha Biopharmaceuticals, Inc. Wuxi 214122, China
*
Authors to whom correspondence should be addressed.
Received: 31 October 2013 / Revised: 12 December 2013 / Accepted: 13 December 2013 / Published: 23 December 2013
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [693 KB, 18 June 2014; original version 18 June 2014]   |  

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. View Full-Text
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 (CC BY 3.0).

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MDPI and ACS Style

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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