Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis
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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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Efflux pump, Indole, MDR-TB, Thioridazine, Tuberculosis
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Inglês
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European Journal of Medicinal Chemistry, v. 127, p. 147-158.
