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

doi:10.1016/j.ejmech.2016.12.042

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Date

2017-01-01

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Article

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

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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.

How to cite this document

Scalacci, Nicolï¿½ et al. Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. European Journal of Medicinal Chemistry, v. 127, p. 147-158. Available at: <http://hdl.handle.net/11449/178534>.