Molecules with N-oxide functionalities are omnipresent in nature and play an important role in Medicinal Chemistry. They are synthetic or biosynthetic intermediates, prodrugs, drugs, or polymers for applications in drug development and surface engineering. Typically, the N-oxide group is critical for biomedical applications of these molecules. It may provide water solubility or decrease membrane permeability or immunogenicity. In other cases, the N-oxide has a special redox reactivity which is important for drug targeting and/or cytotoxicity. Many of the underlying mechanisms have only recently been discovered, and the number of applications of N-oxides in the healthcare field is rapidly growing. This Perspective article gives a short summary of the properties of N-oxides and their synthesis. It also provides a discussion of current applications of N-oxides in the biomedical field and explains the basic molecular mechanisms responsible for their biological activity.

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具有氮氧化物官能团的药物的药物化学

具有N-氧化物官能团的分子在自然界中无处不在，并在药物化学中发挥着重要作用。它们是用于药物开发和表面工程的合成或生物合成中间体、前药、药物或聚合物。通常，N-氧化物基团对于这些分子的生物医学应用至关重要。它可以提供水溶性或降低膜渗透性或免疫原性。在其他情况下，N-氧化物具有特殊的氧化还原反应性，这对于药物靶向和/或细胞毒性很重要。许多潜在机制最近才被发现， N-氧化物在医疗保健领域的应用数量正在快速增长。这篇观点文章对N-氧化物的性质及其合成进行了简短总结。它还讨论了氮氧化物在生物医学领域的当前应用，并解释了其生物活性的基本分子机制。