Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics

We have developed a first generation of hybrid sparsomycin–linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant Gram-positive bacteria as well as the fastidious Gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis. The convergent synthesis of these new compounds is detailed.

We have developed a first generation of hybrid sparsomycin–linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant Gram-positive bacteria as well as the fastidious Gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis. The convergent synthesis of these new compounds is detailed.Figure optionsDownload as PowerPoint slide