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.
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|Titolo:||Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis|
|Citazione:||Scalacci, N., Brown, A.K., Pavan, F.R., Ribeiro, C.M., MANETTI, F., Bhakta, S., et al. (2017). Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 127, 147-158.|
|Appare nelle tipologie:||1.1 Articolo in rivista|