Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2
Basic Information
ID: ALA4699433
Journal: RSC Med Chem
Title: Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2
Authors: Kirk, R., Ratcliffe, A., Noonan, G., Uosis-Martin, M., Lyth, D., Bardell-Cox, O., Massam, J., Schofield, P., Lyons, A., Clare, D., Maclean, J., Smith, A., Savage, V., Mohmed, S., Charrier, C., Salisbury, A-M., Moyo, E., Ooi, N., Chalam-Judge, N., Cheung, J., Stokes, N. R., Best, S., Craighead, M., Armer, R., Huxley, A.
Abstract: Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC90 of 0.5 microg 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.
CiteXplore: 34095845
DOI: 10.1039/d0md00175a
Patent ID: ┄