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Molecules. 2013 Dec 23;19(1):102-21. doi: 10.3390/molecules19010102.

1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.

Author information

1
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. wwenlong2011@163.com.
2
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. jli@mail.shcnc.ac.cn.
3
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China. fanwenhua1987@163.com.

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.

PMID:
24366088
DOI:
10.3390/molecules19010102
[Indexed for MEDLINE]
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