Synthesis and antiplasmodial evaluation of novel (4-aminobutyloxy)quinolines

S. Vandekerckhove, C. Mueller, D. Vogt, C. Lategan, P.J. Smith, K. Chibale, N. Kimpe, de, M.W.A. D'hooghe

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    20 Citations (Scopus)


    A variety of 5-, 6- and 8-(4-aminobutyloxy)quinolines as novel oxygen analogues of known 4- and 8-(4-aminobutylamino)quinoline antimalarial drugs was generated from hydroxyquinolines through a three-step approach with a rhodium-catalyzed hydroformylation as the key step. Antiplasmodial assays of these new quinolines revealed micromolar potency for all representatives against a chloroquine-sensitive strain of Plasmodium falciparum, and three compounds showed submicromolar activity against a chloroquine-resistant strain of P. falciparum with IC50-values ranging between 150 and 680 nM.
    Original languageEnglish
    Pages (from-to)318-322
    JournalBioorganic and Medicinal Chemistry Letters
    Issue number1
    Publication statusPublished - 2013


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