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On the search for potential anti-Trypanosoma cruzi drugs: Synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactions

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dc.contributor.authorSilva Junior, Eufranio N. da
dc.contributor.authorMelo, Isadora M. M. de
dc.contributor.authorDiogo, Emilay B. T.
dc.contributor.authorCosta, Verenice A.
dc.contributor.authorSouza Filho, Jose D. de
dc.contributor.authorValenca, Wagner O.
dc.contributor.authorCamara, Celso A.
dc.contributor.authorOliveira, Ronaldo N. de
dc.contributor.authorAraujo, Alexandre S. de [UNESP]
dc.contributor.authorEmery, Flavio S.
dc.contributor.authorSantos, Marcelo R. dos
dc.contributor.authorSimone, Carlos A. de
dc.contributor.authorMenna-Barreto, Rubem F. S.
dc.contributor.authorCastro, Solange L. de
dc.contributor.institutionUniversidade Federal de Minas Gerais (UFMG)
dc.contributor.institutionUniversidade Federal Rural de Pernambuco (UFRPE)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade de Brasília (UnB)
dc.contributor.institutionFiocruz MS
dc.date.accessioned2014-05-20T14:02:32Z
dc.date.available2014-05-20T14:02:32Z
dc.date.issued2012-06-01
dc.description.abstractFive 2-hydroxy-3-substituted-aminomethyl naphthoquinones, nine 1,2,3-triazolic para-naphthoquinones, five nor-beta-lapachone-based 1,2,3-triazoles, and several other naphthoquinonoid compounds were synthesized and evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease, continuing our screening program for new trypanocidal compounds. Among all the substances, 16-18, 23, 25-29 and 30-33 were herein described for the first time and fifteen substances were identified as more potent than the standard drug benznidazole, with IC50/24 h values in the range of 10.9-101.5 mu M. Compounds 14 and 19 with Selectivity Index of 18.9 and 6.1 are important structures for further studies. (C) 2012 Elsevier B.V. All rights reserved.en
dc.description.affiliationUniversidade Federal de Minas Gerais (UFMG), Lab Quim Sintet & Heterocicl, Inst Ciencias Exatas, Dept Quim, BR-31270901 Belo Horizonte, MG, Brazil
dc.description.affiliationUniversidade Federal Rural de Pernambuco (UFRPE), Dept Ciencias Mol, BR-52171900 Recife, PE, Brazil
dc.description.affiliationUNESP, Inst Biociencias Letras & Ciencias Exatas Sao Jos, Dept Fis, BR-15054000 Sao Jose do Rio Preto, SP, Brazil
dc.description.affiliationUniv São Paulo, Fac Ciencias Farmaceut, BR-14040903 São Paulo, Brazil
dc.description.affiliationUniversidade de Brasilia (UnB), Inst Quim, BR-70910970 Brasilia, DF, Brazil
dc.description.affiliationUniv São Paulo, Dept Fis & Informat, Inst Fis, BR-13560160 São Carlos, SP, Brazil
dc.description.affiliationFiocruz MS, Lab Biol Celular, Inst Oswaldo Cruz, BR-21045900 Rio de Janeiro, RJ, Brazil
dc.description.affiliationUnespUNESP, Inst Biociencias Letras & Ciencias Exatas Sao Jos, Dept Fis, BR-15054000 Sao Jose do Rio Preto, SP, Brazil
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipFundação de Amparo à Ciência e Tecnologia do Estado de Pernambuco (FACEPE)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ)
dc.description.sponsorshipINCT_if
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipIdFAPEMIG: APQ-04166-10
dc.description.sponsorshipIdFAPESP: 09/14184-0
dc.description.sponsorshipIdFAPESP: 09/51812-0
dc.description.sponsorshipIdPRONEM-FACEPE: APQ-232106/10
dc.description.sponsorshipIdFAPERJ: E-26/110.574/2010
dc.description.sponsorshipIdFAPERJ: 101.579/2010
dc.format.extent304-312
dc.identifierhttp://dx.doi.org/10.1016/j.ejmech.2012.03.039
dc.identifier.citationEuropean Journal of Medicinal Chemistry. Paris: Elsevier B.V., v. 52, p. 304-312, 2012.
dc.identifier.doi10.1016/j.ejmech.2012.03.039
dc.identifier.issn0223-5234
dc.identifier.urihttp://hdl.handle.net/11449/22044
dc.identifier.wosWOS:000304291600030
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.ispartofjcr4.816
dc.relation.ispartofsjr1,266
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectNaphthoquinonesen
dc.subjectLapacholen
dc.subjectChagas diseaseen
dc.subjectTrypanosoma cruzien
dc.subjectChemotherapyen
dc.titleOn the search for potential anti-Trypanosoma cruzi drugs: Synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactionsen
dc.typeArtigo
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier B.V.
dspace.entity.typePublication
unesp.author.lattes2044157599722078[9]
unesp.author.orcid0000-0001-9376-9748[9]
unesp.campusUniversidade Estadual Paulista (UNESP), Instituto de Biociências, Letras e Ciências Exatas, São José do Rio Pretopt
unesp.departmentFísica - IBILCEpt

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São José do Rio Preto - IBILCE - Instituto de Biociências, Letras e Ciências Exatas