School of Food and Biological Engineering, Key Laboratory of Metabolism and Regulation for Major Diseases of Anhui Higher Education Institutes, Hefei University of Technology, Hefei, Anhui, 230601, China.
Department of Pharmacy, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, 230001, China.
Curr Top Med Chem. 2020;20(28):2535-2577. doi: 10.2174/1568026620999200917153856.
Thiazole is an important 5-membered heterocyclic compound containing nitrogen and sulfur atoms with various pharmaceutical applications including anti-inflammatory, anti-cancer, anti-viral, hypoglycemic, anti-bacterial and anti-fungal activities. Until now, the FDA-approved drugs containing thiazole moiety have achieved great success such as dasatinib and dabrafenib. In recent years, considerable research has been focused on thiazole derivatives, especially 2,4,5-trisubstituted thiazole derivatives, due to their multiple medicinal applications. This review covers related literature in the past 20 years, which reported the 2,4,5-trisubstituted thiazole as a privileged scaffold in drug design and activity improvement. Moreover, this review aimed to provide greater insights into the rational design of more potent pharmaceutical molecules based on 2,4,5-trisubstituted thiazole in the future.
噻唑是一种重要的含氮和硫原子的五元杂环化合物，具有多种药物应用，包括抗炎、抗癌、抗病毒、降血糖、抗菌和抗真菌活性。到目前为止，含有噻唑部分的 FDA 批准药物已经取得了巨大的成功，如达沙替尼和达拉非尼。近年来，由于其多种药用用途，噻唑衍生物，特别是 2,4,5-三取代噻唑衍生物，受到了相当多的关注。这篇综述涵盖了过去 20 年的相关文献，这些文献报道了 2,4,5-三取代噻唑作为药物设计和活性改善的优势骨架。此外，本综述旨在为未来基于 2,4,5-三取代噻唑设计更有效力的药物分子提供更深入的见解。
Zotero 插件