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The discovery of naturally occurring monocyclic \u03b2\u2010lactams in the late 1970s, mainly active against aerobic Gram\u2010negative bacteria, has introduced a new approach in the design and development of novel antibacterial \u03b2\u2010lactam agents. The main goal was the derivatization of the azetidin\u20102\u2010one core in order to improve their antibacterial potency, broaden their spectrum of activity, and enhance their \u03b2\u2010lactamase stability. In that respect, our review covers the updates in the field of monocyclic \u03b2\u2010lactam 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 \u03b2\u2010lactams, classified according to their <jats:italic>N<\/jats:italic>\u2010substituent, and the associated antibacterial or \u03b2\u2010lactamase inhibitory activities is provided. The different paragraphs disclose a number of well\u2010established 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 \u03b2\u2010lactams and concludes by highlighting the recent developments on siderophore\u2010conjugated classes of monocyclic \u03b2\u2010lactams.<\/jats:p>","DOI":"10.1002\/med.21443","type":"journal-article","created":{"date-parts":[[2017,8,17]],"date-time":"2017-08-17T07:22:56Z","timestamp":1502954576000},"page":"426-503","source":"Crossref","is-referenced-by-count":101,"title":["Antibacterial and \u03b2\u2010Lactamase Inhibitory Activity of Monocyclic \u03b2\u2010Lactams"],"prefix":"10.1002","volume":"38","author":[{"given":"Lena","family":"Decuyper","sequence":"first","affiliation":[{"name":"SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering Ghent University  Ghent 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