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

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 20 , Issue 28 , 2020


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Graphical Abstract:


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.

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