N. Scalacci
Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis
Scalacci, N.; Brown, A.K.; Pavan, F.R.; Ribeiro, C.M.; Manetti, F.; Bhakta, S.; Maitra, A.; Smith, D.L.; Petricci, E.; Castagnolo, D.
Authors
A.K. Brown
F.R. Pavan
C.M. Ribeiro
F. Manetti
S. Bhakta
A. Maitra
D.L. Smith
E. Petricci
D. Castagnolo
Abstract
The neuroleptic drug thioridazine has been recently repositioned as possible anti-tubercular drug. Thioridazine showed anti-tubercular activity against drug resistant mycobacteria but it is endowed with adverse side effects. A small library of thioridazine derivatives has been designed through the replacement of the piperidine and phenothiazine moieties, with the aim to improve the anti-tubercular activity and to reduce the cytotoxic effects. Among the resulting compounds, the indole derivative 12e showed an antimycobacterial activity significantly better than thioridazine and a cytotoxicity 15-fold lower.
Citation
Scalacci, N., Brown, A., Pavan, F., Ribeiro, C., Manetti, F., Bhakta, S., …Castagnolo, D. (2017). Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. European Journal of Medicinal Chemistry, 127, 147-158. https://doi.org/10.1016/j.ejmech.2016.12.042
Journal Article Type | Article |
---|---|
Acceptance Date | Dec 21, 2016 |
Online Publication Date | Dec 23, 2016 |
Publication Date | Feb 15, 2017 |
Deposit Date | Mar 7, 2017 |
Publicly Available Date | Dec 23, 2017 |
Journal | European Journal of Medicinal Chemistry |
Print ISSN | 0223-5234 |
Publisher | Elsevier |
Peer Reviewed | Peer Reviewed |
Volume | 127 |
Pages | 147-158 |
DOI | https://doi.org/10.1016/j.ejmech.2016.12.042 |
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http://creativecommons.org/licenses/by-nc-nd/4.0/
Copyright Statement
© 2016 This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
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