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Current Topics in Medicinal Chemistry

Author(s): Zhen Zhang, Bing Shu, Yaodong Zhang*, Girdhar Singh Deora * and Qing-Shan Li*

DOI: 10.2174/1568026620999200917153856

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

Page: [2535 - 2577] Pages: 43

  • * (Excluding Mailing and Handling)

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.

Graphical Abstract

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