1. Academic Validation
  2. Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2

Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2

  • RSC Med Chem. 2020 Sep 18;11(12):1379-1385. doi: 10.1039/d0md00175a.
R Kirk 1 A Ratcliffe 1 G Noonan 1 M Uosis-Martin 1 D Lyth 1 O Bardell-Cox 1 J Massam 1 P Schofield 1 A Lyons 1 D Clare 1 J Maclean 1 A Smith 1 V Savage 1 S Mohmed 1 C Charrier 1 A-M Salisbury 1 E Moyo 1 N Ooi 1 N Chalam-Judge 1 J Cheung 1 N R Stokes 1 S Best 1 M Craighead 1 R Armer 1 A Huxley 1
Affiliations

Affiliation

  • 1 Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
Abstract

Building on our previously-reported novel tricyclic Topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC90 of 0.5 μg 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.

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