Overcoming resistance to β-lactam antibiotics

Abstract

β-Lactam antibiotics are one of the most important antibiotic classes but are plagued by problems of resistance, and the development of new β-lactam antibiotics through side-chain modification of existing β-lactam classes is not keeping pace with resistance development. In this JOCSynopsis, we summarize small molecule strategies to overcome resistance to β-lactam antibiotics. These approaches include the development of β-lactamase inhibitors and compounds that interfere with the ability of the bacteria to sense an antibiotic threat and activate their resistance mechanisms.

Figure 1

Structures of the different β-lactam antibiotic classes

Figure 2

New β-lactamase inhibitors

Figure 3

Compounds that potentiate β-lactam antibiotic activity by interfering with cell wall biosynthesis.

Figure 4

Compounds that potentiate β-lactam antibiotic activity by affecting antibiotic resistance activation pathways