Departamento de Quimica Organica, Programa de Pos-Graduacao em Quimica, Universidade Federal Fluminense, Outeiro de Sao Joao Baptista, 24020-141 Niteroi, RJ, Brazil.
Departamento de Tecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal Fluminense, R. Dr. Mario Vianna, 523, Santa Rosa, , CEP 24241-002, Niteroi-RJ, Brazil.
Curr Top Med Chem. 2018;18(17):1428-1453. doi: 10.2174/1568026618666180821143902.
Heterocyclic rings having nitrogen atoms are the molecular fragments most used in drug design by using the tools of medicinal chemistry. The 1,2,4-triazole rings are part of an extensive family of drugs that are in use in the pharmaceutical market. More recently, 1,2,3-triazole rings have begun to arouse the great interest of scientists and therefore, many researches have been developed seeking the synthesis of new substances and their possible biological activities. A number of articles have been published by us and others highlighting the synthetic and biological aspects of 1,2,3-triazoles. The growth of new substances of this class was largely due to the simple and selective synthetic method of 1,2,3- triazole ring developed by Sharpless et al. However, some 1,2,3-triazole cannot be synthesized by this method. This review focuses on other synthetic methods that give access to other variations around the 1,2,3-triazole core. The systematic arrangement in this review explores the possibility of providing practical guidance to alternatives of this heterocycle. It has been divided into sections according to the types of starting materials and reactions.
具有氮原子的杂环环是药物设计中使用药物化学工具最常使用的分子片段。1,2,4-三唑环是在药物市场中使用的广泛的药物家族的一部分。最近，1,2,3-三唑环开始引起科学家的极大兴趣，因此，已经开展了许多研究来寻求新物质的合成及其可能的生物活性。我们和其他人发表了许多文章，强调了 1,2,3-三唑的合成和生物学方面。该类新物质的增长在很大程度上归因于 Sharpless 等人开发的简单且选择性的 1,2,3-三唑环合成方法。然而，有些 1,2,3-三唑不能用这种方法合成。这篇综述重点介绍了其他合成方法，这些方法可以获得 1,2,3-三唑核心周围的其他变化。本综述的系统排列根据起始材料和反应的类型探索了提供这种杂环替代物的实际指导的可能性。它已根据起始材料和反应的类型分为几节。
