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噻唑环在临床批准药物中的应用与合成

Application and synthesis of thiazole ring in clinically approved drugs.

作者信息

Niu Zhen-Xi, Wang Ya-Tao, Zhang Sheng-Nan, Li Yan, Chen Xiao-Bing, Wang Sai-Qi, Liu Hong-Min

机构信息

Department of Pharmacy, Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, 450018, China.

First People's Hospital of Shangqiu, Henan Province, Shangqiu, 476100, China; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, China.

出版信息

Eur J Med Chem. 2023 Mar 15;250:115172. doi: 10.1016/j.ejmech.2023.115172. Epub 2023 Feb 1.

Abstract

The development of heterocyclic derivatives has progressed considerably over the past few decades, and many new agents of synthetic and natural origin have been produced. Among heterocyclic compounds, thiazole is a unique five-membered heterocyclic motif characterized by nitrogen and sulfur atoms, which is widely used as an important core skeleton in a variety of pharmaceutically important compounds due to their diverse biological activities, such as antibacterial, antivirus, and antifungal. To the best of our knowledge, more than 90 thiazole-containing derivatives have been currently under clinical investigation, and some thiazole analogs have been approved to treat various diseases. As the potentially privileged scaffolds, thiazole derivatives can be further extensively explored to search for new drugs characterized by improved therapeutic efficacy and similar biological targets. This review aims to outline the applications and synthetic routes of some representative thiazole-containing drugs approved in the clinic, which may guide medicinal researchers to rationally design more effective thiazole-containing drug candidates.

摘要

在过去几十年中,杂环衍生物的发展取得了显著进展,已经生产出许多合成和天然来源的新药物。在杂环化合物中,噻唑是一种独特的五元杂环结构,其特征在于氮原子和硫原子,由于其具有多种生物活性,如抗菌、抗病毒和抗真菌活性,它被广泛用作各种具有重要药学意义的化合物中的重要核心骨架。据我们所知,目前有90多种含噻唑衍生物正在进行临床研究,一些噻唑类似物已被批准用于治疗各种疾病。作为潜在的优势骨架,噻唑衍生物可以进一步广泛探索,以寻找具有更高治疗效果和相似生物靶点的新药。本综述旨在概述一些已在临床上获批的代表性含噻唑药物的应用和合成路线,这可能会指导药物研究人员合理设计更有效的含噻唑候选药物。

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