Dual β-lactam-fluoroquinolone compounds: a novel approach to antibacterial treatment

Abstract

Codrugs comprise a β-lactam-fluoroquinolone antibacterial hybrid. These new agents have been developed with the aim of enhancing the antibacterial spectrum of current therapies, overcoming intrinsic and acquired resistance, and diminishing severe side-effects. A few compounds, including Ro 23-9424, have entered Phase I clinical trials. Furthermore, a series of oral codrugs have been synthesised, although clear oral bioavailability has not yet been demonstrated. New drugs are urgently needed to treat Gram-positive resistant bacteria.

• dual cephalosporin-quinolone
• dual penem-quinolone
• Ro 23-9424