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European Journal of Medicinal Chemistry
Vol. 97, 2015, Pages: 699–718

Recent applications of 1,3-thiazole core structure in the identification of new lead compounds and drug discovery

Adile Ayati, Saeed Emami, Ali Asadipour, Abbas Shafiee, Alireza Foroumadi

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.


1,3-Thiazole is one of the most important scaffolds in heterocyclic chemistry and drug design and discovery. It is widely found in diverse pharmacologically active substances and in some naturally-occurring compounds. Thiazole is a versatile building-block for lead generation, and is easily access of diverse derivatives for subsequent lead optimization. In the recent years, many thiazole derivatives have been synthesized and subjected to varied biological activities. In this article we intended to review the most important biological effects of thiazole-based compounds and highlight their roles in new leads identification and drug discovery. This article is also intended to help researches for finding potential future directions on the development of more potent and specific analogs of thiazole-based compounds for various biological targets.

Graphical abstract

Keywords: Thiazole; Antimicrobials; Anti-cancer; Antioxidants; Anti-inflammatory; Anticonvulsants; Enzyme inhibitors; Lead compounds.

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