Thiazole-based and thiazolidine-based protein tyrosine phosphatase 1B inhibitors as potential anti-diabetes agents
- PDF / 3,116,567 Bytes
- 16 Pages / 595.276 x 790.866 pts Page_size
- 11 Downloads / 165 Views
Medicinal Chemistry Research https://doi.org/10.1007/s00044-020-02668-4
REVIEW ARTICLE
Thiazole-based and thiazolidine-based protein tyrosine phosphatase 1B inhibitors as potential anti-diabetes agents Kexin Chen1,2 Xu Yao1 Ting Tang1 Li-Mei Chen1 Can Xiao1 Jing-Yi Wang1 Hong-Fei Chen1 Zhong-Xing Jiang2 Yi Liu1 Xing Zheng 1 ●
●
●
●
●
●
●
●
●
1234567890();,:
1234567890();,:
Received: 8 August 2020 / Accepted: 6 November 2020 © Springer Science+Business Media, LLC, part of Springer Nature 2020
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 antidiabetes activity. Keywords Diabetes PTP1B Insulin resistance Thiazoles Thiazolidines ●
●
●
●
Introduction
These authors contributed equally: Kexin Chen, Xu Yao Co-first author: Xu Yao * Zhong-Xing Jiang [email protected] * Yi Liu [email protected] * Xing Zheng [email protected] 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
2
Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071 Hubei, China
Protein tyrosine phosphorylation is one of the most crucial mechanisms for regulating cell functions, which is a reversible process controlled by protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs). PTKs can transfer phosphate, while PTPs are responsible for catalyzing the hydro
Data Loading...
