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

Lookup NU author(s): Dr Alistair Brown, Dr Darren Smith

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This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (CC BY-NC-ND).


Abstract

© 2016 Elsevier Masson SAS 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.


Publication metadata

Author(s): Scalacci N, Brown AK, Pavan FR, Ribeiro CM, Manetti F, Bhakta S, Maitra A, Smith DL, Petricci E, Castagnolo D

Publication type: Article

Publication status: Published

Journal: European Journal of Medicinal Chemistry

Year: 2017

Volume: 127

Pages: 147-158

Print publication date: 15/02/2017

Online publication date: 23/12/2016

Acceptance date: 21/12/2016

Date deposited: 26/06/2018

ISSN (print): 0223-5234

ISSN (electronic): 1768-3254

Publisher: Elsevier Masson SAS

URL: https://doi.org/10.1016/j.ejmech.2016.12.042

DOI: 10.1016/j.ejmech.2016.12.042

PubMed id: 28039773


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