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

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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.

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

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Article information


Submitted
25 May 2020
Accepted
07 Aug 2020
First published
18 Sep 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

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 and A. Huxley, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/D0MD00175A

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