Rational Design, Synthesis And Testing Of Novel Tricyclic Topoisomerase Inhibitors For The Treatment Of Bacterial Infections Part 2

Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC90 of 0.5 mu g mL(-1) against Staphylococcus aureus, favourable in vitro pharmacokinetic properties, selectivity versus human topoisomerase II and an acceptable toxicity profile. The results herein validate a rational design approach to address the urgent unmet medical need for novel antibiotics.