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

Stephanie Vandekerckhove, Christian Muller, Dieter Vogt, Carmen Lategan, Peter J. Smith, Kelly Chibale, Norbert De Kimpe, Matthias D'hooghe

Research output: Contribution to journalArticlepeer-review

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 languageEnglish
Pages (from-to)318-322
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Volume23
Issue number1
DOIs
Publication statusPublished - 1 Jan 2013

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