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.

糖尿病是与代谢综合征密切相关的疾病，已成为严重影响许多人生活质量的公共卫生问题。寻找新型抗糖尿病药仍然是控制这种具有挑战性的疾病的基石。酪氨酸磷酸酶1B（PTP1B）是胰岛素和瘦素信号通路的负调节剂，已被证明是II型糖尿病（T2DM）和肥胖症的潜在靶标。近年来，基于PTP1B抑制剂的新型抗糖尿病药物的开发引起了许多研究人员的关注。噻唑是一种含有硫和氮原子的五元杂环，被认为是各种活性化合物的基本核心骨架。此外，噻唑烷类化合物代表一系列带有饱和噻唑环的化合物，天然存在于具有多种药理活性的天然产物和合成化合物中。在这里，我们将重点放在PTP1B在糖尿病中的重要性以及在过去十年中基于噻唑和噻唑烷衍生物的PTP1B抑制剂的开发。已经详细阐述了许多PTP1B抑制剂及其化学结构，选择性，效价和构效关系。这篇综述中描述的绝大多数含有噻唑和噻唑烷部分的PTP1B抑制剂均表现出较好的活性，这对于具有抗糖尿病活性的PTP1B抑制剂的合理设计和有效应用至关重要。在过去的十年中，我们重点研究了PTP1B在糖尿病中的重要性以及基于噻唑和噻唑烷衍生物的PTP1B抑制剂的开发。已经详细阐述了许多PTP1B抑制剂及其化学结构，选择性，效价和构效关系。这篇综述中描述的绝大多数含有噻唑和噻唑烷部分的PTP1B抑制剂均表现出较好的活性，这对于具有抗糖尿病活性的PTP1B抑制剂的合理设计和有效应用至关重要。在过去的十年中，我们重点研究了PTP1B在糖尿病中的重要性以及基于噻唑和噻唑烷衍生物的PTP1B抑制剂的开发。已经详细阐述了许多PTP1B抑制剂及其化学结构，选择性，效价和构效关系。这篇综述中描述的绝大多数含有噻唑和噻唑烷部分的PTP1B抑制剂均表现出较好的活性，这对于具有抗糖尿病活性的PTP1B抑制剂的合理设计和有效应用至关重要。