再次蹭一下2022年诺贝尔化学奖『点击化学』的热度。
点击化学在药物发现领域有着非常大的应用前景。2019年，山东大学药学院刘新泳、展鹏、康东伟等人发表了 Recent applications of click chemistry in drug discovery 综述，详细介绍了近年来点击化学在药物发现领域的研究进展。
机翻摘要：
简介：过去，点击化学已被广泛用于加速铅的发现和优化。点击化学在过去已被广泛利用，以加快线索的发现和优化。事实上，铜催化的叠氮-烷基环化反应（CuAAC）点击化学是一种生物正交反应，在整个药物化学和化学生物学中有着广泛的应用。
专家意见：点击化学反应是药物化学工具箱的重要组成部分，在克服有用化学合成的局限性、提高产量和改善化合物库的质量方面，为药物化学家提供了实质性的优势。为了探索含有高度结构多样性的类药分子的新的化学空间，将以多样性为导向的合成和 "特权 "的基于子结构的策略与生物正交反应合并起来，利用复杂的自动化和流动系统来提高生产率，可能是有用的。以这种方式获得的大型化合物库对发现生物活性化合物和治疗药物应该有很大价值。
摘要原文：
Introduction: Click chemistry has been exploited widely in the past to expedite lead discovery and optimization. Indeed, Copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry is a bioorthogonal reaction of widespread utility throughout medicinal chemistry and chemical biology.
Areas covered: The authors review recent applications of CuAAC click chemistry to drug discovery based on the literature published since 2013. Furthermore, the authors provide the reader with their expert perspectives on the area including their outlook on future developments.
Expert opinion: Click chemistry reactions are an important part of the medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms of overcoming the limitations of useful chemical synthesis, increasing throughput, and improving the quality of compound libraries. To explore new chemical spaces for drug-like molecules containing a high degree of structural diversity, it may be useful to merge the diversity-oriented synthesis and ‘privileged’ substructure-based strategy with bioorthogonal reactions using sophisticated automation and flow systems to improve productivity. Large compound libraries obtained in this way should be of great value for the discovery of bioactive compounds and therapeutic agents.