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Type: Artigo
Title: Synthesis Of Xylitan Derivatives And Preliminary Evaluation Of In Vitro Trypanocidal Activity
Author: Elias
Paula Regina; Coelho
Gleicekelly Silva; Xavier
Viviane Flores; Sales Junior
Policarpo Ademar; Romanha
Alvaro Jose; Fonseca Murta
Silvane Maria; Carneiro
Claudia Martins; Camilo
Nilton Soares; Hilario
Flaviane Francisco; Taylor
Jason Guy
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.
Subject: Xylitan
In Vitro
Chagas Disease
Editor: MDPI AG
Citation: Molecules. Mdpi Ag, v. 21, p. , 2016.
Rights: aberto
Identifier DOI: 10.3390/molecules21101342
Date Issue: 2016
Appears in Collections:Unicamp - Artigos e Outros Documentos

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