Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis

Página do item simplificado
dc.contributor.authorScalacci, Nicol�
dc.contributor.authorBrown, Alistair K.
dc.contributor.authorPavan, Fernando R. [UNESP]
dc.contributor.authorRibeiro, Camila M. [UNESP]
dc.contributor.authorManetti, Fabrizio
dc.contributor.authorBhakta, Sanjib
dc.contributor.authorMaitra, Arundhati
dc.contributor.authorSmith, Darren L.
dc.contributor.authorPetricci, Elena
dc.contributor.authorCastagnolo, Daniele
dc.contributor.institutionKing's College London
dc.contributor.institutionNorthumbria University Newcastle
dc.contributor.institutionQueens Campus
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionDipartimento di Biotecnologie
dc.contributor.institutionUniversity of London
dc.date.accessioned2018-12-11T17:30:49Z
dc.date.available2018-12-11T17:30:49Z
dc.date.issued2017-01-01
dc.description.abstractThe 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.en
dc.description.affiliationInstitute of Pharmaceutical Science King's College London, 150 Stamford Street
dc.description.affiliationNorthumbria University Newcastle Department of Applied Sciences, Ellison Building, Ellison Place
dc.description.affiliationSchool of Medicine Pharmacy and Health Durham University Wolfson Research Institute Queens Campus, Stockton on Tees
dc.description.affiliationS�o Paulo State University (UNESP) School of Pharmaceutical Sciences
dc.description.affiliationDipartimento di Biotecnologie, Chimica e Farmacia, Via A. Moro 2
dc.description.affiliationMycobacteria Research Laboratory Department of Biological Sciences Institute of Structural and Molecular Biology University of London, Birkbeck, Malet Street
dc.description.affiliationUnespS�o Paulo State University (UNESP) School of Pharmaceutical Sciences
dc.description.sponsorshipRoyal Society of Chemistry
dc.format.extent147-158
dc.identifierhttp://dx.doi.org/10.1016/j.ejmech.2016.12.042
dc.identifier.citationEuropean Journal of Medicinal Chemistry, v. 127, p. 147-158.
dc.identifier.doi10.1016/j.ejmech.2016.12.042
dc.identifier.file2-s2.0-85007140997.pdf
dc.identifier.issn1768-3254
dc.identifier.issn0223-5234
dc.identifier.scopus2-s2.0-85007140997
dc.identifier.urihttp://hdl.handle.net/11449/178534
dc.language.isoeng
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.ispartofsjr1,266
dc.rights.accessRightsAcesso aberto
dc.sourceScopus
dc.subjectEfflux pump
dc.subjectIndole
dc.subjectMDR-TB
dc.subjectThioridazine
dc.subjectTuberculosis
dc.titleSynthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosisen
dc.typeArtigo
unesp.departmentCiências Biológicas - FCFpt

Arquivos

Pacote Original

Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
2-s2.0-85007140997.pdf
Tamanho:
1009.78 KB
Formato:
Adobe Portable Document Format
Descrição:
Baixar

Coleções

Araraquara - FCF - Faculdade de Ciências Farmacêuticas