Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700

Several potent oxazolidinone antibacterial agents were obtained by systematic modification of the linker between the five-membered heterocycle and the piperazinyl ring of RBx 7644 (Ranbezolid, 1) and its thienyl analogue 2, leading to the identification of an expanded spectrum compound RBx 8700 (6b).

Graphical abstractThe potent broad spectrum oxazolidinone antibacterial agent RBx 8700 (6b) was obtained by systematic modification of the methylene linker of RBx 7644 (Ranbezolid, 1) and its thienyl analogue 2.Figure optionsDownload full-size imageDownload as PowerPoint slide