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Thiazole-based and thiazolidine-based protein tyrosine phosphatase 1B inhibitors as potential anti-diabetes agents

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Abstract

As a disease closely related to the metabolic syndrome, diabetes has become a public health issue that severely affects many people’s quality of life. The search for novel anti-diabetic agents remains the cornerstone to control this challenging disease. Protein tyrosine phosphatase 1B (PTP1B), a negative regulator of insulin and leptin signaling pathways, has turned out to be a potential target of type II diabetes mellitus (T2DM) and obesity. In recent years, the development of novel anti-diabetic drugs based on PTP1B inhibitors has captured the attention of many researchers. Thiazole, a five-membered heterocycle containing sulfur and nitrogen atoms, has been considered as an essential core skeleton for various active compounds. Furthermore, thiazolidines, representing a series of compounds with saturated thiazole rings, widely exist in natural products and synthetic compounds with a variety of pharmacological activities. Here, we focus on the emphasis of PTP1B in diabetes and the development of PTP1B inhibitors based on thiazole and thiazolidine derivatives in the past decade. Many PTP1B inhibitors and their chemical structures, selectivity, potency, and structure-activity relationship have been elaborated. The great majority of PTP1B inhibitors containing thiazole and thiazolidine moieties described in this review exhibit preferable activities, which would be of importance for the rational design and efficient application of PTP1B inhibitors with anti-diabetes activity.

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Acknowledgements

The authors thank the Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (2018-10), the Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study (0223-0007-000004), the Undergraduate Research Learning and Innovative Experiment Project (G201910555028, S201910555024, S201910555143, X2019177, X2019178, X2019179, 2018XJXZ349, 2018XJXZ350, 2018XJXZ351, 2018XJXZ360, 2018XJXZ363), Hunan Provincial Hengyang Joint Fund (2020JJ6052), Program for Innovative Talent Team of Hengyang (2017-1), the Key Project of Hengyang Science and Technology Department (2017KJ166) for financial support.

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  1. These authors contributed equally: Kexin Chen, Xu Yao

Authors and Affiliations

  1. Group of Lead Compound, Department of Pharmacy, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, the Second Affiliated Hospital of University of South China, Hengyang, 421001, Hunan, China

    Kexin Chen, Xu Yao, Ting Tang, Li-Mei Chen, Can Xiao, Jing-Yi Wang, Hong-Fei Chen, Yi Liu & Xing Zheng

  2. Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, Hubei, China

    Kexin Chen & Zhong-Xing Jiang

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  1. Kexin Chen
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  2. Xu Yao
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  3. Ting Tang
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  4. Li-Mei Chen
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  5. Can Xiao
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  6. Jing-Yi Wang
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  7. Hong-Fei Chen
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  8. Zhong-Xing Jiang
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  9. Yi Liu
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  10. Xing Zheng
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Corresponding authors

Correspondence to Zhong-Xing Jiang, Yi Liu or Xing Zheng.

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Co-first author: Xu Yao

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Chen, K., Yao, X., Tang, T. et al. Thiazole-based and thiazolidine-based protein tyrosine phosphatase 1B inhibitors as potential anti-diabetes agents. Med Chem Res 30, 519–534 (2021). https://doi.org/10.1007/s00044-020-02668-4

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  • DOI: https://doi.org/10.1007/s00044-020-02668-4

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