beta-Lactams and beta-Lactamase Inhibitors: An Overview.

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Bush K, Bradford PA

beta-Lactams and beta-Lactamase Inhibitors: An Overview.

Cold Spring Harb Perspect Med. 2016 Aug 1;6(8). pii: cshperspect.a025247. doi: 10.1101/cshperspect.a025247.

PubMed ID
27329032 [ View in PubMed
]
Abstract

beta-Lactams are the most widely used class of antibiotics. Since the discovery of benzylpenicillin in the 1920s, thousands of new penicillin derivatives and related beta-lactam classes of cephalosporins, cephamycins, monobactams, and carbapenems have been discovered. Each new class of beta-lactam has been developed either to increase the spectrum of activity to include additional bacterial species or to address specific resistance mechanisms that have arisen in the targeted bacterial population. Resistance to beta-lactams is primarily because of bacterially produced beta-lactamase enzymes that hydrolyze the beta-lactam ring, thereby inactivating the drug. The newest effort to circumvent resistance is the development of novel broad-spectrum beta-lactamase inhibitors that work against many problematic beta-lactamases, including cephalosporinases and serine-based carbapenemases, which severely limit therapeutic options. This work provides a comprehensive overview of beta-lactam antibiotics that are currently in use, as well as a look ahead to several new compounds that are in the development pipeline.

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