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  • Title: Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3.
    Author: Vellasco Junior WT, Guedes GP, Vasconcelos TR, Vaz MG, de Souza MV, Krettli AU, Krettli LG, Aguiar AC, Gomes CR, Cunico W.
    Journal: Eur J Med Chem; 2011 Nov; 46(11):5688-93. PubMed ID: 21982338.
    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.
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