Design, Synthesis, and Trypanocidal Activity of Novel 5-Nitroimidazolyl O-Benzyloxime Ethers

dc.creatorCarvalho, Samir Aquino
dc.creatorOsorio, Luis Felipe Baumotte
dc.creatorSalomão, Kelly
dc.creatorCastro, Solange Lisboa de
dc.creatorWardell, Solange M. S. V.
dc.creatorWardell, James Lewis
dc.creatorSilva, Edson Ferreira da
dc.creatorFraga, Carlos Alberto Manssour
dc.date2018-06-21T16:20:55Z
dc.date2018-06-21T16:20:55Z
dc.date2017
dc.date.accessioned2023-09-26T23:56:50Z
dc.date.available2023-09-26T23:56:50Z
dc.identifierCARVALHO, Samir Aquino; et al. Design, Synthesis, and Trypanocidal Activity of Novel 5-Nitroimidazolyl O-Benzyloxime Ethers. Journal of Heterocyclic Chemistry, v. 54, n. 3626, p. 1-6, 2017.
dc.identifier0022-152X
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/27046
dc.identifier10.1002/jhet.2989
dc.identifier1943-5193
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8895880
dc.descriptionIn this paper, we describe the synthesis and the action against of the trypomastigote form of Trypanosoma cruzi of a new class of nitroimidazole-2-carbaldehyde O-benzyloximes. These derivatives were designed through the application of molecular hybridization concept between two potent antiprotozoal compounds, the 5-nitrothiophene-2-carbaldehyde O-oxime 6 and the trypanocidal piperidinyl-4-carbaldehyde Obenzyloxime 7 with the intention of reaching two distinct molecular targets of T. cruzi. The activity of these benzyl ether derivatives was tested against the infective trypomastigote forms of T. cruzi, and the derivative (E)-1-methyl-5-nitro-1H-imidazole-2-carbaldehyde O-(4-nitrobenzyl) oxime (1) presented moderate trypanocidal activity (IC50 = 12.7 μM) when compared with the standard drug benznidazole, which showed to be a good starting point for the design of more effective trypanocide agents.
dc.description2030-01-01
dc.formatapplication/pdf
dc.languageeng
dc.publisherWiley
dc.rightsrestricted access
dc.subjectTripanossomicidas
dc.subjectSintese
dc.subjectAtividade dos tripanossomicidas
dc.subjectÈteres
dc.subjectTrypanocidal Activity
dc.subjectDesign
dc.subjectSynthesis
dc.subjectNovel 5-Nitroimidazolyl O-Benzyloxime Ethers
dc.titleDesign, Synthesis, and Trypanocidal Activity of Novel 5-Nitroimidazolyl O-Benzyloxime Ethers
dc.typeArticle


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