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

Journal: RSC medicinal chemistry
Published Date:

Abstract

Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC of 0.5 μg mL against , favourable pharmacokinetic properties, selectivity 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.

Authors

  • R Kirk
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • A Ratcliffe
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • G Noonan
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • M Uosis-Martin
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • D Lyth
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • O Bardell-Cox
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • J Massam
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • P Schofield
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • A Lyons
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • D Clare
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • J Maclean
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • A Smith
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • V Savage
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • S Mohmed
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • C Charrier
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • A-M Salisbury
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • E Moyo
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • N Ooi
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • N Chalam-Judge
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • J Cheung
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • N R Stokes
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • S Best
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • M Craighead
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • R Armer
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.
  • A Huxley
    Redx Anti-Infectives Ltd Alderley Park Macclesfield SK10 4TG Cheshire UK.

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