Synthesis of Xylitan Derivatives and Preliminary Evaluation of in Vitro Trypanocidal Activity
AbstractA 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. View Full-Text
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Elias, P.R.; Coelho, G.S.; Xavier, V.F.; Sales Junior, P.A.; Romanha, A.J.; Murta, S.M.F.; Carneiro, C.M.; Camilo, N.S.; Hilário, F.F.; Taylor, J.G. Synthesis of Xylitan Derivatives and Preliminary Evaluation of in Vitro Trypanocidal Activity. Molecules 2016, 21, 1342.
Elias PR, Coelho GS, Xavier VF, Sales Junior PA, Romanha AJ, Murta SMF, Carneiro CM, Camilo NS, Hilário FF, Taylor JG. Synthesis of Xylitan Derivatives and Preliminary Evaluation of in Vitro Trypanocidal Activity. Molecules. 2016; 21(10):1342.Chicago/Turabian Style
Elias, Paula R.; Coelho, Gleicekelly S.; Xavier, Viviane F.; Sales Junior, Policarpo A.; Romanha, Alvaro J.; Murta, Silvane M.F.; Carneiro, Claudia M.; Camilo, Nilton S.; Hilário, Flaviane F.; Taylor, Jason G. 2016. "Synthesis of Xylitan Derivatives and Preliminary Evaluation of in Vitro Trypanocidal Activity." Molecules 21, no. 10: 1342.
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