Novel benzamido derivatives as PTP1B inhibitors with anti-hyperglycemic and lipid-lowering efficacy

Based on a non-competitive and selective PTP1B inhibitor reported by us previously, thirty-nine benzamido derivatives were designed and synthesized as novel PTP1B inhibitors. Among them, twelve compounds exhibited IC values at micromolar level against human recombinant PTP1B, and most of them exhibi...

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Published in:Acta pharmaceutica Sinica. B 2018-10, Vol.8 (6), p.919-932
Main Authors: Tang, Yanbo, Zhang, Xiaolin, Chen, Zheng, Yin, Wenwen, Nan, Guanglei, Tian, Jinying, Ye, Fei, Xiao, Zhiyan
Format: Article
Language:English
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Summary:Based on a non-competitive and selective PTP1B inhibitor reported by us previously, thirty-nine benzamido derivatives were designed and synthesized as novel PTP1B inhibitors. Among them, twelve compounds exhibited IC values at micromolar level against human recombinant PTP1B, and most of them exhibited significant selectivity to PTP1B over TC-PTP and CD45. Further evaluation of the most potent compound on high-fat diet (HFD)-induced insulin-resistant (IR) obese mice indicated that could modulate glucose metabolism and ameliorate dyslipidemia simultaneously.
ISSN:2211-3835
2211-3843
DOI:10.1016/j.apsb.2018.05.001