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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.

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Authors

N. Scalacci

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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