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Lookup NU author(s): Yucheng Lu, Daniel Partleton, Musa Gugu, Ahmed Alhejaili, Dr Jonathan Harburn, Dr Jason GillORCiD, Dr Jon Sellars, Dr Alistair BrownORCiD
This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).
© 2025 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.Despite efforts to discover effective treatments to eradicate tuberculosis (TB), it remains a global threat. The increase in drug-resistant bacterial species has made the discovery of new drugs highly coveted. The utilisation of previous efficacious structures is one approach that can be employed to developing novel series of compounds to combat this ever-growing problem. This study sought to re-examine two such compounds, isoxyl (ISO) and SQ109, previously shown to be efficacious in TB treatment. SQ109-ISO hybrid compounds were shown to have demonstrable activity against both drug-sensitive and drug-resistant Mtb whilst displaying limited toxicity in vitro in comparison to other antitubercular agents. Indications from our genetic and biochemical studies suggest that these structurally similar pharmacophores bind to different proteins within Mtb, highlighting the need for careful consideration when producing regioisomeric analogues and that the utilisation of previous efficacious structures is a valid approach to developing promising novel drugs against Mtb.
Author(s): Lu Y, Partleton D, Gugu FM, Alhejaili AYG, Norris S, Harburn JJ, Gill JH, Sellars JD, Brown AK
Publication type: Article
Publication status: Published
Journal: Journal of Enzyme Inhibition and Medicinal Chemistry
Year: 2025
Volume: 40
Issue: 1
Online publication date: 21/05/2025
Acceptance date: 23/04/2025
Date deposited: 09/06/2025
ISSN (print): 1475-6366
ISSN (electronic): 1475-6374
Publisher: Taylor and Francis Ltd.
URL: https://doi.org/10.1080/14756366.2025.2502600
DOI: 10.1080/14756366.2025.2502600
Data Access Statement: the main text and the supplementary Material contain all the nec- essary data to evaluate this study’s conclusions. additional data generated during the current study are available from the corresponding author upon reasonable request.
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