Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
Scalacci, N. and Brown, A.K. and Pavan, F.R. and Ribeiro, C.M. and Manetti, F. and Bhakta, Sanjib and Maitra, Arundhati and Smith, D.L. and Petricci, E. and Castagnolo, D. (2017) Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. European Journal of Medicinal Chemistry 127 , pp. 147-158. ISSN 0223-5234.
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Abstract
The neuroleptic drug thioridazine has been recently repositioned as possible antitubercular drug. Thioridazine showed antitubercular 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 antitubercular 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.
Metadata
| Item Type: | Article |
|---|---|
| School: | Birkbeck Faculties and Schools > Faculty of Science > School of Natural Sciences |
| Depositing User: | Arundhati Maitra |
| Date Deposited: | 24 Jan 2017 16:13 |
| Last Modified: | 02 Aug 2023 17:31 |
| URI: | https://eprints.bbk.ac.uk/id/eprint/17993 |
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