Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi

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dc.contributor.authorArenas Velasquez, Angela Maria [UNESP]
dc.contributor.authorFrancisco, Acacio Ivo
dc.contributor.authorNakaima Kohatsu, Andrea Akiko [UNESP]
dc.contributor.authorJesus Silva, Flavia Alves de [UNESP]
dc.contributor.authorRodrigues, Danilo Fernando [UNESP]
dc.contributor.authorSilva Teixeira, Rafaela Gomes da
dc.contributor.authorChiari, Bruna Galdorfini [UNESP]
dc.contributor.authorJose de Almeida, Maria Gabriela [UNESP]
dc.contributor.authorIsaac, Vera Lucia Borges [UNESP]
dc.contributor.authorVargas, Maria D.
dc.contributor.authorCicarelli, Regina Maria Barretto [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade Federal Fluminense (UFF)
dc.date.accessioned2014-12-03T13:11:43Z
dc.date.available2014-12-03T13:11:43Z
dc.date.issued2014-04-01
dc.description.abstractTrypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1, N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl, N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells. (c) 2014 Elsevier Ltd. All rights reserved.en
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Araraquara, Brazil
dc.description.affiliationUniv Estadual Paulista, Inst Quim, BR-14800900 Araraquara, Brazil
dc.description.affiliationUniv Fed Fluminense, Inst Quim, BR-24020150 Niteroi, RJ, Brazil
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, BR-14801902 Araraquara, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Araraquara, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Inst Quim, BR-14800900 Araraquara, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, BR-14801902 Araraquara, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipFundação para o Desenvolvimento da UNESP (FUNDUNESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.format.extent1707-1710
dc.identifierhttp://dx.doi.org/10.1016/j.bmcl.2014.02.046
dc.identifier.citationBioorganic & Medicinal Chemistry Letters. Oxford: Pergamon-elsevier Science Ltd, v. 24, n. 7, p. 1707-1710, 2014.
dc.identifier.doi10.1016/j.bmcl.2014.02.046
dc.identifier.issn0960-894X
dc.identifier.lattes4842462513285606
dc.identifier.urihttp://hdl.handle.net/11449/113461
dc.identifier.wosWOS:000333567600016
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofBioorganic & Medicinal Chemistry Letters
dc.relation.ispartofjcr2.442
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectSleeping sicknessen
dc.subjectChagas diseaseen
dc.subjectBenzyl diaminesen
dc.subjectFerrocenyl diaminesen
dc.titleSynthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzien
dc.typeArtigo
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier B.V.
unesp.author.lattes4842462513285606
unesp.author.orcid0000-0002-1295-9046[3]
unesp.author.orcid0000-0003-0762-6199[5]
unesp.author.orcid0000-0001-7959-0207[7]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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Artigos - Ciências Biológicas - FCFAR
Artigos - Fármacos e Medicamentos - FCFAR