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Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors

Du, X.; Zhang, S.-E.; Liu, J.-Z.; Nie, F.-L.; Ye, F.; Tian, J.-Y.; Xiao, Z.-Y.

Yao Xue Xue Bao 47(3): 367-373

2012

ISSN/ISBN: 0513-4870
PMID: 22645761
Document Number: 658672
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.

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