β-内酰胺酶抑制剂研究进展

细菌耐药问题日益严峻，已经引起了公众的广泛关注。β-内酰胺类抗生素是应用最广的抗生素，但是细菌对此类药物的耐药严重降低了药物的治疗效果，而产生β-内酰胺酶是β-内酰胺类药物耐药的主要机制，研制β-内酰胺酶抑制剂，以此作为增效剂与β-内酰胺类抗生素联用，可有效恢复细菌对β-内酰胺类药物的敏感性。临床上广泛传播的β-内酰胺酶有丝氨酸β-内酰胺酶和金属β-内酰胺酶。目前，在增效剂的研究中，已经获得了多种有效的丝氨酸β-内酰胺酶抑制剂，许多金属β-内酰胺酶抑制剂仍处于研究阶段。此外，为了应对由多种β-内酰胺酶引起的多重感染，研发丝氨酸β-内酰胺酶/金属β-内酰胺酶双重抑制剂也是逆转β-内酰胺类抗生素耐药性的新思路。本文综述了β-内酰胺酶抑制剂的研究进展，为研制新型β-内酰胺酶抑制剂提供借鉴。

Research progress on β-lactamase inhibitors

The growing problem of bacterial resistance has caused widespread public concerns. β-Lactam antibiotics are the most widely used antibiotics, but the bacterial resistance severely reduces the therapeutic effects of drugs, and β-lactamases is the main mechanism of β-lactam resistance. The development of β-lactamase inhibitors and its use as a synergist with β-lactam antibiotics can effectively restore bacterial sensitivity to β-lactam drugs. Clinically widely disseminated β-lactamases are serine β-lactamases and metallo β-lactamases. At present, a variety of effective serine β-lactamases inhibitors have been obtained in the study of synergists, and many metallo β-lactamases inhibitors are still in the research stage. In addition, in order to cope with multiple infections of a variety of β-lactamases, the discovery of serine β-lactamases/metallo β-lactamases dual inhibitors is also a new way to reverse the resistance of β-lactam antibiotics. This article reviews the research progress of β-lactamase inhibitors and provides references for the development of novel β-lactamase