Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/23184
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dc.contributor.authorSilva, Ari Miranda
dc.contributor.authorSilva, Leonardo Araújo
dc.contributor.authorBombaça, Ana Cristina S.
dc.contributor.authorMenna-Barreto, Rubem F. S.
dc.contributor.authorSantos, Claudio Eduardo Rodrigues
dc.contributor.authorFerreira, Aurélio B. Buarque
dc.contributor.authorCastro, Solange L. de
dc.date.accessioned2017-11-14T15:42:23Z
dc.date.available2017-11-14T15:42:23Z
dc.date.issued2017
dc.identifier.citationSILVA, Ari Miranda da; et al. Synthesis and biological evaluation of N-alkyl naphthoimidazoles derived from β-lapachone against Trypanosoma cruzi bloodstream trypomastigotes. Med. Chem. Commun., v.8, p.952-959, 2017.
dc.identifier.issn2040-2503
dc.identifier.urihttps://www.arca.fiocruz.br/handle/icict/23184
dc.language.isoeng
dc.publisherRoyal Society of Chemistry
dc.rightsrestricted access
dc.subject.otherTrypanosoma cruzi
dc.subject.otherRelação Quantitativa Estrutura-Atividade
dc.subject.otherDoença de Chagas
dc.titleSynthesis and biological evaluation of N-alkyl naphthoimidazoles derived from β-lapachone against Trypanosoma cruzi bloodstream trypomastigotes
dc.typeArticle
dc.description.abstractenThe QSAR study of 34 2-aryl-naphthoimidazoles screened so far revealed that σi is the most important factor for their lytic activity on the bloodstream trypomastigote forms of T. cruzi, the etiologic agent of Chagas disease. Based on this result, 16 new N-alkyl-naphthoimidazoles derived from 6,6-dimethyl- 3,4,5,6-tetrahydrobenzoij7,8]chromeneij5,6-d]imidazole (the product of the reaction of β-lapachone with paraformaldehyde) by its reaction with halo-alkanes were prepared and evaluated against the parasite and peritoneal macrophages. The N1-n-hexyl and N3-n-hexyl naphthoimidazoles were 2.2 and 3.2 times more active than the standard drug benznidazole with selectivity indices of 2.7 and 13.4, respectively.
dc.creator.affilliationUniversidade Federal Rural do Rio de Janeiro. Programa de Pós-graduação em Química.. Seropédica, RJ, Brasil / Universidade Federal do Rio de Janeiro. Instituto de Pesquisas em Produtos Naturais. Rio de Janeiro, RJ, Brasill.
dc.creator.affilliationUniversidade Federal Rural do Rio de Janeiro. Programa de Pós-graduação em Química.. Seropédica, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
dc.creator.affilliationUniversidade Federal Rural do Rio de Janeiro. Programa de Pós-graduação em Química.. Seropédica, RJ, Brasil.
dc.creator.affilliationUniversidade Federal Rural do Rio de Janeiro. Programa de Pós-graduação em Química.. Seropédica, RJ, Brasil.
dc.creator.affilliationFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
dc.subject.enTrypanosoma cruzi
dc.subject.enQSAR
dc.subject.enChagas Disease
dc.subject.enN-alkyl naphthoimidazoles
dc.subject.enβ-lapachone
dc.identifier.eissn2040-2511
Appears in Collections:IOC - Artigos de Periódicos

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