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Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: Anti-Mycobacterium tuberculosis activity and cytotoxicity

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dc.contributor.authorPavan, Fernando Rogério [UNESP]
dc.contributor.authorMaia, Pedro I. da S.
dc.contributor.authorLeite, Sergio R. A. [UNESP]
dc.contributor.authorDeflon, Victor M.
dc.contributor.authorBatista, Alzir A.
dc.contributor.authorSato, Daisy N.
dc.contributor.authorFranzblau, Scott G.
dc.contributor.authorLeite, Clarice Queico Fujimura [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade Federal de São Carlos (UFSCar)
dc.contributor.institutionInstituto Adolfo Lutz (IAL)
dc.contributor.institutionUniv Illinois
dc.date.accessioned2014-05-20T13:24:14Z
dc.date.available2014-05-20T13:24:14Z
dc.date.issued2010-05-01
dc.description.abstractThe aim of this study was to identify a candidate drug for the development of anti-tuberculosis therapy from previously synthesized compounds based on the thiosemicarbazones, semicarbazones, dithio-carbazates and hydrazide/hydrazones compounds. The minimal inhibitory concentration (MIC) of these compounds against Mycobacterium tuberculosis was determined. Their in vitro cytotoxicity to J774 cells (IC(50)) was determined to establish a selectivity index (SI) (SI = IC(50)/MIC). The best compounds were the thiosemicarbazones (2, 3 and 4) and the hydrazide/hydrazones (14, 15, 16 and 18). The results are comparable to or better than those of "first line" or "second line" drugs commonly used to treat TB, suggesting these compounds as anti-TB drug candidates. (C) 2010 Elsevier Masson SAS. All rights reserved.en
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUniv São Paulo, Inst Quim São Carlos, BR-1356659 São Carlos, SP, Brazil
dc.description.affiliationUniv Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP, Brazil
dc.description.affiliationUniversidade Federal de São Carlos (UFSCar), Dept Quim, BR-13565905 São Carlos, SP, Brazil
dc.description.affiliationInst Adolfo Lutz Registro, Unidade Ribeirao Preto, BR-14085410 Ribeirao Preto, SP, Brazil
dc.description.affiliationUniv Illinois, Coll Pharm, Inst TB Res, Chicago, IL USA
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP, Brazil
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 08/10390-2
dc.description.sponsorshipIdFAPESP: 09/06499-1
dc.format.extent1898-1905
dc.identifierhttp://dx.doi.org/10.1016/j.ejmech.2010.01.028
dc.identifier.citationEuropean Journal of Medicinal Chemistry. Paris: Elsevier France-editions Scientifiques Medicales Elsevier, v. 45, n. 5, p. 1898-1905, 2010.
dc.identifier.doi10.1016/j.ejmech.2010.01.028
dc.identifier.issn0223-5234
dc.identifier.lattes2114570774349859
dc.identifier.urihttp://hdl.handle.net/11449/7460
dc.identifier.wosWOS:000276695200025
dc.language.isoeng
dc.publisherElsevier France-editions Scientifiques Medicales Elsevier
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.ispartofjcr4.816
dc.relation.ispartofsjr1,266
dc.rights.accessRightsAcesso restritopt
dc.sourceWeb of Science
dc.subjectAntimycobacterial agentsen
dc.subjectREMAen
dc.subjectCytotoxicityen
dc.subjectThiosemicarbazonesen
dc.subjectSemicarbazonesen
dc.subjectDithiocarbazatesen
dc.subjectHydrazide/hydrazonesen
dc.titleThiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: Anti-Mycobacterium tuberculosis activity and cytotoxicityen
dc.typeArtigopt
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier France-editions Scientifiques Medicales Elsevier
dspace.entity.typePublication
relation.isDepartmentOfPublication5004bcab-94af-4939-b980-091ae9d0a19e
relation.isDepartmentOfPublication.latestForDiscovery5004bcab-94af-4939-b980-091ae9d0a19e
relation.isOrgUnitOfPublication95697b0b-8977-4af6-88d5-c29c80b5ee92
relation.isOrgUnitOfPublication.latestForDiscovery95697b0b-8977-4af6-88d5-c29c80b5ee92
unesp.author.lattes2114570774349859
unesp.author.orcid0000-0002-6969-3963[1]
unesp.author.orcid0000-0002-8698-0243[7]
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentCiências Biológicas - FCFpt

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Araraquara - FCF - Faculdade de Ciências Farmacêuticas