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dc.contributor.authorMicheletti, Ana Camila
dc.contributor.authorHonda, Neli Kika
dc.contributor.authorPavan, Fernando Rogério [UNESP]
dc.contributor.authorLeite, Clarice Queico Fujimura [UNESP]
dc.contributor.authorCepa Matos, Maria de Fatima
dc.contributor.authorPerdomo, Renata Trentin
dc.contributor.authorBogo, Danielle
dc.contributor.authorAlcantara, Glaucia Braz
dc.contributor.authorBeatriz, Adilson
dc.date.accessioned2014-12-03T13:09:12Z
dc.date.available2014-12-03T13:09:12Z
dc.date.issued2013-11-01
dc.identifierhttp://dx.doi.org/10.2174/1573406411309070003
dc.identifier.citationMedicinal Chemistry. Sharjah: Bentham Science Publ Ltd, v. 9, n. 7, p. 904-910, 2013.
dc.identifier.issn1573-4064
dc.identifier.urihttp://hdl.handle.net/11449/112072
dc.description.abstractA new dihydropyranexanthone derived from the natural xanthone lichexanthone (1) was synthesised and, together with other 18 derivatives including omega-bromo and omega-aminoalkoxylxanthones (containing methyl, ethyl, propyl, tert-butylamino and piperidinyl moieties), were tested against Mycobacterium tuberculosis. Nine omega-aminoalkoxylxanthones showed good antimycobacterial activity, and their in vitro cytotoxicity was determined using VERO cells in order to calculate the selectivity index (SI). One of these nitrogenated xanthone derivatives showed very promising results, with MIC of 2.6 mu M and SI of 48. This MIC is comparable to values found in first and second line drugs commonly used to treat TB. In order to understand better about this compound, it was evaluated together with two other ones that showed good SI, against resistant clinical strains of M. tuberculosis to verify the existence of cross-resistance. A chemometrical approach was useful to establish a pattern of antitubercular activity among the group of -aminoalkoxylxanthones, according to some structural and chemical features.en
dc.description.sponsorshipFUNDECT/MS
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipPROPP-UFMS
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.format.extent904-910
dc.language.isoeng
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofMedicinal Chemistry
dc.sourceWeb of Science
dc.subjectChemometricsen
dc.subjectlichenen
dc.subjectstructural modificationsen
dc.subjecttuberculosisen
dc.subjectxanthoneen
dc.titleIncrement of Antimycobaterial Activity on Lichexanthone Derivativesen
dc.typeArtigo
dcterms.rightsHolderBentham Science Publ Ltd
dc.contributor.institutionUniversidade Federal de Mato Grosso do Sul (UFMS)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.description.affiliationUniv Fed Mato Grosso do Sul, Ctr Ciencias Exatas & Tecnol, Campo Grande, MS, Brazil
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUniv Fed Mato Grosso do Sul, Ctr Ciencias Biol & Saude, Campo Grande, MS, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.identifier.wosWOS:000326089300002
dc.rights.accessRightsAcesso restrito
dc.description.sponsorshipIdFAPESP: 08/10390-2
dc.description.sponsorshipIdFAPESP: 09/06499-1
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt
dc.identifier.lattes2114570774349859
unesp.author.lattes2114570774349859
unesp.author.orcid0000-0002-6969-3963[3]
unesp.author.orcid0000-0001-6864-6092[9]
dc.relation.ispartofjcr2.631
dc.relation.ispartofsjr0,372
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