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

Nicolò Scalacci, Alistair Brown, Fernando Pavan, Camila Ribeiro, Fabrizio Manetti, Sanjib Bhakta, Arundhati Maitra, Darren Smith, Elena Petricci, Daniele Castagnolo

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)147-158
JournalEuropean Journal of Medicinal Chemistry
Volume127
Early online date23 Dec 2016
DOIs
Publication statusPublished - 15 Feb 2017

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