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

AbstractAs 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 (T 2DM) 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 c ompounds. 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 b ased 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 thi s review exhibit preferable activities, which would be of importance for the rational design and efficient application of PTP1B inhibitors with anti-diabete...
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research