期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 212, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.113069
关键词
Click reaction; Anti-proliferatives; Anti-plasmodials; Anti-tuberculars; Anti-microbials; Structure-activity relationship
1H-1,2,3-triazole, obtained through the Click Reaction, has become a favorite among synthetic/medicinal chemists for its ability to mimic different functional groups and enhance targeted biological activities. Triazole derivatives have shown potential in accelerating the development of new scaffolds and are essential in biomolecular mimetics and fragment-based drug design.
The continuous demand of medicinally important scaffolds has prompted the synthetic chemists to identify simple and efficient routes for their synthesis. 1H-1,2,3-triazole, obtained by highly versatile, efficacious and selective Click Reaction has become a synthetic/medicinal chemist's favorite not only because of its ability to mimic different functional groups but also due to enhancement in the targeted biological activities. Triazole ring has also been shown to play a critical role in biomolecular mimetics, fragment-based drug design, and bioorthogonal methodologies. In addition, the availability of triazole containing drugs such as fluconazole, furacyclin, etizolam, voriconazole, triozolam etc. in market has underscored the potential of this biologically enriched core in expediting development of new scaffolds. The present review, therefore, is an attempt to highlight the recent synthetic/biological advancements in triazole derivatives that could facilitate the in-depth understanding of its role in the drug discovery process. (C) 2020 Published by Elsevier Masson SAS.
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