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

R. Kirk; A. Ratcliffe; G. Noonan; M. Uosis-Martin; D. Lyth; O. Bardell-Cox; J. Massam; P. Schofield; A. Lyons; D. Clare; J. Maclean; A. Smith; V. Savage; S. Mohmed; C. Charrier; A-M. Salisbury; E. Moyo; N. Ooi; N. Chalam-Judge; J. Cheung; N. R. Stokes; S. Best; M. Craighead; R. Armer; A. Huxley

doi:10.1039/D0MD00175A

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

R. Kirk,

*^a A. Ratcliffe,^a G. Noonan,^a M. Uosis-Martin,^a D. Lyth,^a O. Bardell-Cox,^a J. Massam,^a P. Schofield,^a A. Lyons,^a D. Clare,^a J. Maclean,^a A. Smith,^a V. Savage,

^a S. Mohmed,^a C. Charrier,^a A-M. Salisbury,^a E. Moyo,^a N. Ooi,^a N. Chalam-Judge,^a J. Cheung,^a N. R. Stokes,

^a S. Best,^a M. Craighead,^a R. Armer^a and A. Huxley

*^a

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* Corresponding authors

^a 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.

RSC Medicinal Chemistry

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

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