| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596218 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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 680Â nM.
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Authors
Stéphanie Vandekerckhove, Christian Müller, Dieter Vogt, Carmen Lategan, Peter J. Smith, Kelly Chibale, Norbert De Kimpe, Matthias D'hooghe,