‘β-Lactams’ as β-lactamase inhibitors

Abstract

The application of inhibitors to block the β-lactamase destruction of penicillins and cephalosporins by resistant bacteria is a potentially useful way of improving the efficacy of established compounds. Certain semi-synthetic penicillins and cephalosporins have been found to be competitive inhibitors of selected β-lactamases but an examination of streptomycete culture fluids has revealed two new types of β-lactam compound: clavulanic acid, which is a progressive inactivator of a wide range of β-lactamases, and the olivanic acids, which are both broad-spectrum antibiotics and potent β-lactamase inhibitors. Penicillanic acid sulphone and 6-β-bromopenicillanic acid have been shown to be significant inhibitors of β-lactamase. The chemotherapeutic application of these compounds is discussed.