Bresson Jules, Burke Katie, Ethève-Quelquejeu Mélanie, Iannazzo Laura, Cariou Kevin
Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, Chimie ParisTech, PSL University, CNRS, 11 rue Pierre et Marie Curie, 75005, Paris, France.
Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, Université Paris Cité, CNRS, F-75006, Paris, France.
ChemMedChem. 2025 May 5;20(9):e202400960. doi: 10.1002/cmdc.202400960. Epub 2025 Feb 25.
Antimicrobial resistance is a major public health threat, due to the emergence of new bacterial strains not responding to classical antibiotics. This review focuses on the use of transition metal cross-coupling strategies used to access new β-lactam derivatives, the most well-known and commonly used antibiotics. This manuscript covers the seminal studies for the synthesis of antibiotics up to the current need of accessing specific probes (by functionalizing existing drugs), crucial for the detection of resistances. These strategies also allow the linkage of a cargo to a β-lactam antibiotic for selective release for either therapeutic effect or for diagnostic purposes (in the case of probes), which will be explained in this article.
抗菌耐药性是对公众健康的一大威胁,这是由于出现了对传统抗生素无反应的新型细菌菌株。本综述聚焦于过渡金属交叉偶联策略的应用,该策略用于获取新型β-内酰胺衍生物,β-内酰胺衍生物是最知名且常用的抗生素。本手稿涵盖了从抗生素合成的开创性研究到当前获取特定探针(通过对现有药物进行功能化)的需求,这些探针对于耐药性检测至关重要。这些策略还允许将一种有效载荷与β-内酰胺抗生素连接,以便为治疗效果或诊断目的(在探针的情况下)进行选择性释放,本文将对此进行解释。