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

Scalacci, Nicolò, Brown, Alistair, Pavan, Fernando, Ribeiro, Camila, Manetti, Fabrizio, Bhakta, Sanjib, Maitra, Arundhati, Smith, Darren, Petricci, Elena and Castagnolo, Daniele (2017) Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. European Journal of Medicinal Chemistry, 127. pp. 147-158. ISSN 0223-5234

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Official URL: http://dx.doi.org/10.1016/j.ejmech.2016.12.042

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.

Item Type: Article
Uncontrolled Keywords: Thioridazine; Tuberculosis; MDR-TB; Efflux pump; Indole
Subjects: B900 Others in Subjects allied to Medicine
C500 Microbiology
Department: Faculties > Health and Life Sciences > Applied Sciences
Depositing User: Becky Skoyles
Date Deposited: 09 Jan 2017 09:10
Last Modified: 15 Nov 2017 09:42
URI: http://nrl.northumbria.ac.uk/id/eprint/29043

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