New β-lactam antibiotics and β-lactamase inhibitors.

IMPORTANCE OF THE FIELD

β-Lactam antibiotics are among the most frequently prescribed antibiotics used to treat bacterial infections. However, their utility is being threatened by the worldwide proliferation of β-lactamases with broad hydrolytic capabilities, especially in multidrug-resistant Gram-negative bacteria.

AREAS COVERED IN THIS REVIEW

This review describes new β-lactams and β-lactamase inhibitors described in the patent literature primarily between 2007 and 2010, together with supportive meeting abstracts and relevant descriptive literature.

WHAT THE READER WILL GAIN

Readers will learn which classes of β-lactam antibiotics are being explored as the most promising groups of compounds to counteract resistance in Gram-negative pathogenic bacteria. Somewhat surprisingly, few traditional β-lactam classes such as penicillins or cephalosporins were described in the literature, other than in combinations with other β-lactams or β-lactamase inhibitors that are being developed to inhibit enzymes from all molecular classes.

TAKE HOME MESSAGE

β-Lactam antibiotics are currently being developed as monotherapy by only a few companies. The major emphasis in the past 4 years has been the discovery of novel β-lactamase inhibitors or inhibitor combinations that will allow use of β-lactams against multidrug-resistant bacteria. The use of β-lactams as single agents appears to be a limited option for the future.