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Title: | Synthesis of xylitan derivatives and preliminary evaluation of in vitro trypanocidal activity. |
Authors: | Elias, Paula Regina Coelho, Gleicekelly Silva Xavier, Viviane Flores Sales Júnior, Policarpo Ademar Romanha, Alvaro José Murta, Silvane Maria Fonseca Carneiro, Cláudia Martins Camilo, Nilton Soares Hilário, Flaviane Francisco Taylor, Jason Guy |
Keywords: | Xylitol Anhydropentitol Trypomastigote Chagas disease Amastigote |
Issue Date: | 2016 |
Citation: | ELIAS, P. R. et al. Synthesis of xylitan derivatives and preliminary evaluation of in vitro trypanocidal activity. Molecules, v. 21, p. 1-13, 2016. Disponível em: <http://www.mdpi.com/1420-3049/21/10/1342> Acesso em: 15 set. 2017 |
Abstract: | A series of novel xylitan derivatives derived from xylitol were synthesized using operationally simple procedures. A xylitan acetonide was the key intermediate used to prepare benzoate, arylsulfonate esters and 1,2,3-triazole derivatives of xylitan. These compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as positive control against T. cruzi and cytotoxicity was determined in mammalian L929 cells. The arylsulfonate xylitan derivative bearing a nitro group displayed the best activity of all the compounds tested, and was slightly more potent than the reference drug benznidazole. The importance of the isopropylidene ketal moiety was established and the greater lipophilicity of these compounds suggests enhancement in cell penetration. |
URI: | http://www.repositorio.ufop.br/handle/123456789/11181 |
metadata.dc.identifier.doi: | https://doi.org/10.3390/molecules21101342 |
ISSN: | 1420-3049 |
metadata.dc.rights.license: | This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/). Fonte: o próprio artigo. |
Appears in Collections: | DEQUI - Artigos publicados em periódicos |
Files in This Item:
File | Description | Size | Format | |
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ARTIGO_SynthesisXylitanDerivatives.pdf | 1,13 MB | Adobe PDF | View/Open |
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