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Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.

Scalacci, N. and Brown, A. K. and Pavan, F. R. and Ribeiro, C. M. and Manetti, F. and Bhakta, S. and Maitra, A. and Smith, D. L. and Petricci, E. and Castagnolo, D. (2017) 'Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.', European journal of medicinal chemistry., 127 . pp. 147-158.


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.

Item Type:Article
Full text:(AM) Accepted Manuscript
Available under License - Creative Commons Attribution Non-commercial No Derivatives.
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Publisher statement:© 2016 This manuscript version is made available under the CC-BY-NC-ND 4.0 license
Date accepted:21 December 2016
Date deposited:13 March 2017
Date of first online publication:23 December 2016
Date first made open access:23 December 2017

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