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Kingdon, Alexander, Adcock, Holly V., Kasimati, Eleni-Marina, Craven, Philip, van Schaik, Willem, Cox, Liam R. and Besra, Gurdyal S. (2024) 'Exploration of vanoxerine analogues as antibacterial agents'. The Journal of Antibiotics, Vol 78, Issue 1, pp. 54-63.
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Abstract
Mycobacterium tuberculosis is a bacterial pathogen, responsible for approximately 1.3 million deaths in 2022 through tuberculosis infections. The complex treatment regimen required to treat tuberculosis and growing rates of drug resistance, necessitates the development of new anti-mycobacterial agents. One approach is to repurpose drugs from other clinical applications. Vanoxerine (GBR 12909) was previously shown to have anti-mycobacterial activity, through dissipating the membrane electric potential and hence, cellular energetics. Several vanoxerine analogues were synthesised in this study, which exhibited a range of activities against mycobacteria and enterococcus. All active analogues had similar impacts on the membrane electric potential and inhibition of ethidium bromide efflux. The most active compound displayed reduced inhibitory activity against the known human target of vanoxerine, the dopamine transporter. This work has identified a promising analogue, which could provide a starting point for further medicinal chemistry and drug development efforts to target mycobacteria.
| Item Type: | Article |
|---|---|
| Subjects: | W General Medicine. Health Professions > W 20.5 Biomedical research WF Respiratory System > Tuberculosis > WF 200 Tuberculosis (General) |
| Faculty: Department: | Biological Sciences > Department of Tropical Disease Biology |
| Digital Object Identifer (DOI): | https://doi.org/10.1038/s41429-024-00781-9 |
| SWORD Depositor: | JISC Pubrouter |
| Depositing User: | JISC Pubrouter |
| Date Deposited: | 29 Jan 2025 12:18 |
| Last Modified: | 29 Jan 2025 12:18 |
| URI: | https://archive.lstmed.ac.uk/id/eprint/25949 |
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