Faculty of Chemistry, Lomonosov Moscow State University, Moscow, 119991, Russia.
Biochemistry (Mosc). 2020 Nov;85(11):1292-1309. doi: 10.1134/S0006297920110024.
β-Lactam antibiotics account for about 60% of all produced antibiotics. Due to a high activity and minimal side effects, they are the most commonly used class of antibacterial drugs for the treatment of various infectious diseases of humans and animals, including severe hospital infections. However, the emergence of bacteria resistant to β-lactams has led to the clinical inefficiency of these antibiotics, and as a result, their use in medicine has been limited. The search for new effective ways for overcoming the resistance to β-lactam antibiotics is an essential task. The major mechanism of bacterial resistance is the synthesis of β-lactamases (BLs) that break the antibiotic β-lactam ring. Here, we review specific inhibitors of serine β-lactamases and metallo-β-lactamases and discuss approaches for creating new inhibitors that would prolong the "life" of β-lactams.
β-内酰胺类抗生素约占所有抗生素产量的 60%。由于其高活性和最小的副作用，它们是治疗人类和动物各种传染病的最常用的一类抗菌药物，包括严重的医院感染。然而，细菌对β-内酰胺类抗生素的耐药性的出现导致了这些抗生素在临床上的失效，因此它们在医学上的应用受到了限制。寻找克服β-内酰胺类抗生素耐药性的新有效方法是一项重要任务。细菌耐药的主要机制是合成破坏抗生素β-内酰胺环的β-内酰胺酶（BLs）。在这里，我们综述了丝氨酸β-内酰胺酶和金属β-内酰胺酶的特异性抑制剂，并讨论了创造新抑制剂的方法，以延长β-内酰胺类药物的“寿命”。
