Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors.
- Author:
Xin DU
;
Shuen ZHANG
;
Junzheng LIU
;
Feilin NIE
;
Fei YE
;
Jinying TIAN
;
Zhiyan XIAO
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2012;47(3):367-73
- CountryChina
- Language:Chinese
-
Abstract:
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.
