Due to the widespread emergence of resistant bacterial strains, an urgent need for the development of new antibacterial agents with novel modes of action has emerged. The discovery of naturally occurring monocyclic β‐lactams in the late 1970s, mainly active against aerobic Gram‐negative bacteria, has introduced a new approach in the design and development of novel antibacterial β‐lactam agents. The main goal was the derivatization of the azetidin‐2‐one core in order to improve their antibacterial potency, broaden their spectrum of activity, and enhance their β‐lactamase stability. In that respect, our review covers the updates in the field of monocyclic β‐lactam antibiotics during the last three decades, taking into account an extensive collection of references. An overview of the relationships between the structural features of these monocyclic β‐lactams, classified according to their N‐substituent, and the associated antibacterial or β‐lactamase inhibitory activities is provided. The different paragraphs disclose a number of well‐established classes of compounds, such as monobactams, monosulfactams, monocarbams, monophosphams, nocardicins, as well as other known representative classes. Moreover, this review draws attention to some less common but, nevertheless, possibly important types of monocyclic β‐lactams and concludes by highlighting the recent developments on siderophore‐conjugated classes of monocyclic β‐lactams.

中文翻译：

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单环β-内酰胺的抗菌和β-内酰胺酶抑制活性

由于耐药细菌菌株的广泛出现，迫切需要开发具有新颖作用方式的新型抗菌剂。1970年代末期发现的天然单环β-内酰胺主要对好氧革兰氏阴性菌有活性，为新型抗菌β-内酰胺药物的设计和开发引入了一种新方法。主要目的是将氮杂环丁烷-2-酮核心衍生化，以提高其抗菌效力，拓宽活性范围并增强其β-内酰胺酶稳定性。在这方面，我们的综述涵盖了过去三十年中单环β-内酰胺类抗生素领域的最新进展，同时考虑了广泛的参考文献。提供N取代基，以及相关的抗菌或β-内酰胺酶抑制活性。不同的段落公开了许多公认的化合物类别，例如单bactams，monosulfactams，monocarbams，monophosphams，nocardicins以及其他已知的代表性类别。此外，本综述引起人们对一些较不常见但仍可能重要的单环β-内酰胺类的关注，并通过重点介绍铁载体共轭类单环β-内酰胺类的最新进展来得出结论。