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

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Wen-Long WangBainian Feng

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.

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Citations

Dec 22, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Haibing HeYujun Shi
Feb 5, 2019·Current Topics in Medicinal Chemistry·Phaedra EleftheriouAnthi Petrou

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Methods Mentioned

BETA
NMR

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