Abstract
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 language | English |
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Pages (from-to) | 318-322 |
Number of pages | 5 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 23 |
Issue number | 1 |
DOIs | |
Publication status | Published - 1 Jan 2013 |