Department of Chemistry and Biology "A. Zambelli", University of Salerno, 84084 Fisciano (SA), Italy.
Int J Mol Sci. 2021 Jan 9;22(2):617. doi: 10.3390/ijms22020617.
β-lactam antibiotics are among the most important and widely used antimicrobials worldwide and are comprised of a large family of compounds, obtained by chemical modifications of the common scaffolds. Usually these modifications include the addition of active groups, but less frequently, molecules were synthesized in which either two β-lactam rings were joined to create a single bifunctional compound, or the azetidinone ring was joined to another antibiotic scaffold or another molecule with a different activity, in order to create a molecule bearing two different pharmacophoric functions. In this review, we report some examples of these derivatives, highlighting their biological properties and discussing how this strategy can lead to the development of innovative antibiotics that can represent either novel weapons against the rampant increase of antimicrobial resistance, or molecules with a broader spectrum of action.
β-内酰胺类抗生素是全球最重要和应用最广泛的抗生素之一，它们由一大类化合物组成，这些化合物通过对常见支架的化学修饰而获得。通常，这些修饰包括添加活性基团，但较少见的是，合成了分子，其中要么将两个β-内酰胺环连接在一起形成单一的双功能化合物，要么将氮杂环丁酮环连接到另一个抗生素支架或另一个具有不同活性的分子上，以创建具有两个不同药效基团的分子。在这篇综述中，我们报告了这些衍生物的一些例子，强调了它们的生物学特性，并讨论了这种策略如何导致开发创新的抗生素，这些抗生素可以作为对抗抗菌药物耐药性猖獗增长的新武器，或者具有更广泛作用谱的分子。
