DNA gyrase and topoisomerase IV are known targets in antibacterial drug discovery. Inhibitors of the B subunits of gyrase (GyrB) and topoiosmerase IV (ParE) were designed specifically to block the ATP binding site. The azaindole scaffold was discovered through virtual screening of Kinase/ATP-binding scaffolds. Herein we present synthesis and structure-activity relationship of azaindole-naphthyridone inhibitors of ParE with improved in vivo clearance.

Design, synthesis, and antibacterial activity of azaindole inhibitors of ParE/GyrB with improved properties for the treatment of gram positive bacterial infections

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.