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

DU  Xin

DU Xin, Zhang Shu-En, Liu Jun-Zheng, Nie Fei-Lin, Xie Fei, Tian Jin-Yang, Xiao Zhi-Yan. Design, synthesis and evaluation of malonic acid-based PTP1B inhibitorsJ. 药学学报, 2012,47(3): 367-373.

Citation:

DU Xin, Zhang Shu-En, Liu Jun-Zheng, Nie Fei-Lin, Xie Fei, Tian Jin-Yang, Xiao Zhi-Yan. Design, synthesis and evaluation of malonic acid-based PTP1B inhibitorsJ. 药学学报, 2012,47(3): 367-373.

Citation:

DU Xin, Zhang Shu-En, Liu Jun-Zheng, Nie Fei-Lin, Xie Fei, Tian Jin-Yang, Xiao Zhi-Yan. Design, synthesis and evaluation of malonic acid-based PTP1B inhibitorsJ. 药学学报, 2012,47(3): 367-373.

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

DU Xin

Abstract

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 μmol·L⁻¹, respectively.

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

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