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2,4,5-Trisubstituted Thiazole: A Privileged Scaffold in Drug Design and Activity Improvement

[ Vol. 20 , Issue. 28 ]

Author(s):

Zhen Zhang, Bing Shu, Yaodong Zhang*, Girdhar Singh Deora * and Qing-Shan Li*   Pages 2535 - 2577 ( 43 )

Abstract:


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.

Keywords:

2, 4, 5-trisubstituted thiazole, Biological activity, Structure activity relationships, Supplementary drug design, Antiinflammatory, Anti-cancer.

Affiliation:

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, 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, Henan Provincial Key Laboratory of Children's Genetics and Metabolic Diseases, Children's Hospital Affiliated to Zhengzhou University, Zhengzhou, Henan, 450018, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, 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

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