2,4,5-trisubstituted thiazole: A privileged scaffold in drug design and activity improvement

Zhen Zhang, Bing Shu, Yaodong Zhang, Girdhar Singh Deora, Qing Shan Li

Research output: Contribution to journalReview ArticleResearchpeer-review

6 Citations (Scopus)


Thiazole is an important 5-membered heterocyclic compound containing nitrogen and sulfur atoms with various pharmaceutical applications including anti-inflammatory, anti-cancer, anti-viral, hy-poglycemic, anti-bacterial and anti-fungal activities. Until now, the FDA-approved drugs containing thi-azole 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 im-provement. 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.

Original languageEnglish
Pages (from-to)2535-2577
Number of pages43
JournalCurrent Topics in Medicinal Chemistry
Issue number28
Publication statusPublished - 2020


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

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