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Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3.

Authors: Vellasco, W.T.; Guedes, G.P.; Vasconcelos, T.R.A.; Vaz, M.G.F.; De Souza, M.V.N.; Krettli, A.U.; Krettli, L.G.; Aguiar, A.C.C.; Gomes, C.R.B.; Cunico, W.


Abstract

A series of novel thioetherhydroxyethylsulfonamide derivatives has been synthesized from the coupling of intermediates 3-amino-4-phenyl-1-thioetherazine-butan-2-oles 6,7 with arenesulfonyl chlorides in good yields. Characterizations of products were achieved by NMR techniques and specifically for compound 8e by X-ray crystallography. Preliminary results of antimalarial activity in vitro against the Plasmodium falciparum W2 clone (chloroquine resistant and mefloquine sensitive) showed moderate activity for hydroxyethylsulfonamide 8f. In addition, none of the compounds tested showed cytotoxicity at high concentration tested against HepG2 and BGM cell lines.
Keywords: Hydroxyethylsulfonamides; Thioetherhydroxyethylsulfonamides; Antimalarial
Document Type: Research Article DOI: http://dx.doi.org/10.1016/j.ejmech.2011.09.025 Publication date: 1 de Novembro de 2011

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