In the past few decades, our understanding of glycan information‐encoding power has notably increased, thus leading to a significant growth also in the design and synthesis of glycomimetic probes. Combining data from multiple analytical sources, such as crystallography, nuclear magnetic resonance spectroscopy, and other biophysical methods (eg, surface plasmon resonance and carbohydrate microarrays) has allowed to shed light on the key interaction events between carbohydrates and their protein‐targets. However, the low metabolic stability of carbohydrates and their high hydrophilicity, which translates in low bioavailability, undermine their development as drugs. In this framework, the design of chemically modified analogues (called carbohydrate mimics or glycomimetics) appears as a valid alternative for the development of therapeutic agents. Glycomimetics, as structural and functional mimics of carbohydrates, can replace the native ligands in the interaction with target proteins, but are designed to show enhanced enzymatic stability and bioavailability and, possibly, an improved affinity and selectivity toward the target. In the present account, we specifically focus on the most recent advances in the design and synthesis of glycomimetics. In particular, we highlight the efforts of the scientific community in the development of straightforward synthetic procedures for the preparation of sugar mimics and in their preliminary biological evaluation.

中文翻译：

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糖模拟物的设计和合成：最新进展。

在过去的几十年中，我们对聚糖信息编码能力的理解得到了显着提高，因此在模拟糖探针的设计和合成方面也取得了显着增长。结合来自晶体学，核磁共振波谱和其他生物物理方法（例如，表面等离振子共振和碳水化合物微阵列）等多种分析来源的数据，可以阐明碳水化合物与蛋白质靶标之间的关键相互作用。然而，碳水化合物的低新陈代谢稳定性和其高亲水性转化为低生物利用度，破坏了其作为药物的发展。在这种框架下，化学修饰的类似物（称为碳水化合物模拟物或糖模拟物）的设计似乎是开发治疗剂的有效选择。作为碳水化合物的结构和功能模拟物，糖代谢组学可以代替天然配体与靶蛋白的相互作用，但被设计为显示出增强的酶稳定性和生物利用度，并可能显示出对靶标的更高的亲和力和选择性。在目前的情况下，我们特别关注糖模拟物设计和合成的最新进展。特别是，我们着重强调了科学界在开发用于制备糖模拟物的直接合成程序及其初步生物学评估方面的努力。对目标的亲和力和选择性提高。在目前的帐户中，我们特别关注糖模拟物设计和合成的最新进展。特别是，我们着重强调了科学界在开发用于制备糖模拟物的直接合成程序及其初步生物学评估方面的努力。对目标的亲和力和选择性提高。在目前的帐户中，我们特别关注糖模拟物设计和合成的最新进展。特别是，我们着重强调了科学界在开发用于制备糖模拟物的直接合成程序及其初步生物学评估方面的努力。