Autor(es): Scalacci, Nicol� ; Brown, Alistair K. ; Pavan, Fernando R. [UNESP] ; Ribeiro, Camila M. [UNESP] ; Manetti, Fabrizio ; Bhakta, Sanjib ; Maitra, Arundhati ; Smith, Darren L. ; Petricci, Elena ; Castagnolo, Daniele
Data: 2018
Identificador Persistente: http://hdl.handle.net/11449/178534
Origem: Oasisbr
Assunto(s): Efflux pump; Indole; MDR-TB; Thioridazine; Tuberculosis
Made available in DSpace on 2018-12-11T17:30:49Z (GMT). No. of bitstreams: 0 Previous issue date: 2017-01-01
Royal Society of Chemistry
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.
Institute of Pharmaceutical Science King's College London, 150 Stamford Street
Northumbria University Newcastle Department of Applied Sciences, Ellison Building, Ellison Place
School of Medicine Pharmacy and Health Durham University Wolfson Research Institute Queens Campus, Stockton on Tees
S�o Paulo State University (UNESP) School of Pharmaceutical Sciences
Dipartimento di Biotecnologie, Chimica e Farmacia, Via A. Moro 2
Mycobacteria Research Laboratory Department of Biological Sciences Institute of Structural and Molecular Biology University of London, Birkbeck, Malet Street
S�o Paulo State University (UNESP) School of Pharmaceutical Sciences
