Heterocyclic urea derivatives and methods of use thereof (WO2010142978)

Abstract

A series of ureido derivatives incorporating a highly derivatized quinolone scaffold were prepared by a succession of original steps. The lead molecules of these compounds are the quinolone antibacterials of the nalidixic acid/ciprofloxacin type and they target, similar to these clinically used agents, the DNA gyrase/topoisomerase IV of pathogenic bacteria. These new quinolones are claimed to act as efficient antibacterials against a large number of drug-resistant bacteria such as Staphylococcus spp., Enterococcus spp., Streptococcus spp., Acinetobacter baumannii, Bacteroides bivius, Burkholderia spp., Chlamydia spp., Chlamydophila pneumoniae.

Keywords:

• antibacterial agent
• DNA gyrase
• drug resistance
• phosphate ester; quinolone
• topoisomerase
• urea