| Literature DB >> 28039773 |
Nicolò Scalacci1, Alistair K Brown2, Fernando R Pavan3, Camila M Ribeiro3, Fabrizio Manetti4, Sanjib Bhakta5, Arundhati Maitra5, Darren L Smith6, Elena Petricci4, Daniele Castagnolo7.
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.Entities:
Keywords: Efflux pump; Indole; MDR-TB; Thioridazine; Tuberculosis
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Year: 2016 PMID： 28039773 DOI： 10.1016/j.ejmech.2016.12.042
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514