Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CiQUS), Departamento de Química Orgánica, Universidade de Santiago de Compostela, Jenaro de la Fuente s/n, 15782 Santiago de Compostela, Spain.
Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CiQUS), Departamento de Química Orgánica, Universidade de Santiago de Compostela, Jenaro de la Fuente s/n, 15782 Santiago de Compostela, Spain.
Bioorg Chem. 2024 Sep;150:107528. doi: 10.1016/j.bioorg.2024.107528. Epub 2024 Jun 4.
β-Lactamases are bacterial enzymes that inactivate β-lactam antibiotics and, as such, are the most prevalent cause of antibiotic resistance in Gram-negative bacteria. The ever-increasing production and worldwide dissemination of bacterial strains producing carbapenemases is currently a global health concern. These enzymes catalyze the hydrolysis of carbapenems - the β-lactam antibiotics with the broadest spectrum of activity that are often considered as drugs of last resort. The incidence of carbapenem-resistant pathogens such as Pseudomonas aeruginosa, Acinetobacter baumannii and carbapenemase or extended spectrum beta-lactamase (ESBL)-producing Enterobacterales, which are frequent in clinical settings, is worrisome since, in some cases, no therapies are available. These include all metallo-β-lactamases (VIM, IMP, NDM, SMP, and L1), and serine-carbapenemases of classes A (KPC, SME, IMI, and GES), and of classes D (OXA-23, OXA-24/40, OXA-48 and OXA-58). Consequently, the early diagnosis of bacterial strains harboring carbapenemases is a pivotal task in clinical microbiology in order to track antibiotic bacterial resistance and to improve the worldwide management of infectious diseases. Recent research efforts on the development of chromogenic and fluorescent chemical sensors for the specific and sensitive detection and quantification of β-lactamase production in multidrug-resistant pathogens are summarized herein. Studies to circumvent the main limitations of the phenotypic and molecular methods are discussed. Recently reported chromogenic and fluorogenic cephalosporin- and carbapenem-based β-lactamase substrates will be reviewed as alternative options to the currently available nitrocefin and related compounds, a chromogenic cephalosporin-based reagent widely used in clinical microbiology laboratories. The scope of these new chemical sensors, along with the synthetic approaches to synthesize them, is also summarized.
β-内酰胺酶是细菌产生的酶,可使β-内酰胺类抗生素失活,因此是革兰氏阴性菌中抗生素耐药性的最主要原因。目前,全球范围内越来越多的产碳青霉烯酶细菌菌株的产生和传播令人担忧,这些酶可催化碳青霉烯类抗生素的水解,碳青霉烯类抗生素是具有最广泛活性的β-内酰胺类抗生素,通常被认为是最后一线的药物。在临床环境中经常出现的铜绿假单胞菌、鲍曼不动杆菌和产碳青霉烯酶或扩展谱β-内酰胺酶(ESBL)的肠杆菌科细菌等碳青霉烯类耐药病原体的发生率令人担忧,因为在某些情况下,没有可用的治疗方法。这些酶包括所有金属β-内酰胺酶(VIM、IMP、NDM、SMP 和 L1)、A 类丝氨酸碳青霉烯酶(KPC、SME、IMI 和 GES)和 D 类碳青霉烯酶(OXA-23、OXA-24/40、OXA-48 和 OXA-58)。因此,早期诊断携带碳青霉烯酶的细菌菌株是临床微生物学中的一项关键任务,以便追踪抗生素细菌耐药性并改善全球传染病管理。本文总结了近年来在开发用于检测和定量多药耐药病原体中β-内酰胺酶产生的显色和荧光化学传感器方面的研究进展。讨论了克服表型和分子方法主要局限性的研究。本文将综述最近报道的基于头孢菌素和碳青霉烯的显色和荧光β-内酰胺酶底物,作为目前广泛应用于临床微生物学实验室的硝基头孢菌素和相关化合物的替代选择。还总结了这些新的化学传感器的范围及其合成方法。