GyrB Inhibitors

Chemical Class:
Name of Target:
mycobacterial topoisomerase
A high throughput assay that measures the activity of mycobacterial topoisomerase was developed and used to screen AstraZeneca’s corporate compound collection. Following hit evaluation a number of scaffolds were identified and hit-to-lead work completed. Activity in the mouse model of acute infection (proof-of-concept) was demonstrated, after which the active compounds would provide the lead compound(s) for an optimization effort.