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Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
Scalacci, Nicolò; Brown, Alistair K; Pavan, Fernando R; Ribeiro, Camila M; Manetti, Fabrizio; Bhakta, Sanjib; Maitra, Arundhati; Smith, Darren L; Petricci, Elena; Castagnolo, Daniele.
Afiliação
  • Scalacci N; Institute of Pharmaceutical Science, King's College London, 150 Stamford Street, London, SE1 9NH, United Kingdom; Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, United Kingdom.
  • Brown AK; School of Medicine, Pharmacy and Health, Durham University, Wolfson Research Institute, Queens Campus, Stockton on Tees, TS17 6BH, United Kingdom.
  • Pavan FR; São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, Brazil.
  • Ribeiro CM; São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, Brazil.
  • Manetti F; Dipartimento di Biotecnologie, Chimica e Farmacia, Via A. Moro 2, 53100, Siena, Italy.
  • Bhakta S; Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London, WC1E 7HX, United Kingdom.
  • Maitra A; Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London, WC1E 7HX, United Kingdom.
  • Smith DL; Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, United Kingdom.
  • Petricci E; Dipartimento di Biotecnologie, Chimica e Farmacia, Via A. Moro 2, 53100, Siena, Italy.
  • Castagnolo D; Institute of Pharmaceutical Science, King's College London, 150 Stamford Street, London, SE1 9NH, United Kingdom. Electronic address: daniele.castagnolo@kcl.ac.uk.
Eur J Med Chem ; 127: 147-158, 2017 Feb 15.
Article em En | MEDLINE | ID: mdl-28039773
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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Texto completo: 1 Coleções: 01-internacional Contexto em Saúde: 2_ODS3 / 3_ND Base de dados: MEDLINE Assunto principal: Tioridazina / Desenho de Fármacos / Resistência a Múltiplos Medicamentos / Mycobacterium tuberculosis / Antituberculosos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2017 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Contexto em Saúde: 2_ODS3 / 3_ND Base de dados: MEDLINE Assunto principal: Tioridazina / Desenho de Fármacos / Resistência a Múltiplos Medicamentos / Mycobacterium tuberculosis / Antituberculosos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2017 Tipo de documento: Article