Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, Punjab, India.
Department of Chemistry, Hindu College, Amritsar, Punjab, 143001, India.
Eur J Med Chem. 2021 Feb 15;212:113069. doi: 10.1016/j.ejmech.2020.113069. Epub 2020 Dec 3.
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.
不断增长的对具有医学重要性的支架的需求促使合成化学家确定了它们的合成的简单有效的途径。1H-1,2,3-三唑，通过高多功能、有效和选择性的“点击反应”获得，不仅因为其能够模拟不同的官能团，而且还因为增强了靶向生物活性，已经成为合成/药物化学家的最爱。三唑环也被证明在生物分子模拟、基于片段的药物设计和生物正交方法学中起着关键作用。此外，含有三唑的药物（如氟康唑、呋喃西林、依替唑仑、伏立康唑、三唑仑等）在市场上的出现，强调了这种富含生物的核心在加速新支架开发方面的潜力。因此，本综述旨在强调三唑衍生物在合成/生物学方面的最新进展，这有助于深入了解其在药物发现过程中的作用。
