Application and synthesis of thiazole ring in clinically approved drugs.

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

Journal: European journal of medicinal chemistry 2023;250():115172

PMID: 36758304

Full Text on Elsevier Science View on PubMed

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.

Address: 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.; The Affiliated Cancer Hospital of Zhengzhou University & Henan Cancer Hospital, Henan Engineering Research Center of Precision Therapy of Gastrointestinal Cancer, Zhengzhou Key Laboratory for Precision Therapy of Gastrointestinal Cancer, Zhengzhou, 450008, China. Electronic address: [email protected].; The Affiliated Cancer Hospital of Zhengzhou University & Henan Cancer Hospital, Henan Engineering Research Center of Precision Therapy of Gastrointestinal Cancer, Zhengzhou Key Laboratory for Precision Therapy of Gastrointestinal Cancer, Zhengzhou, 450008, China. Electronic address: [email protected].; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: [email protected].

DOI: 10.1016/j.ejmech.2023.115172