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
  • 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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