New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain

Hidayat Hussain; Sabine Specht; Salem R Sarite; Achim Hoerauf; Karsten Krohn

doi:10.1016/j.ejmech.2012.06.046

New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain

Eur J Med Chem. 2012 Aug:54:936-42. doi: 10.1016/j.ejmech.2012.06.046. Epub 2012 Jul 3.

Authors

Hidayat Hussain¹, Sabine Specht, Salem R Sarite, Achim Hoerauf, Karsten Krohn

Affiliation

¹ Department of Chemistry, University of Paderborn, Warburger Strasse 100, 33098 Paderborn, Germany. Hidayat110@gmail.com

PMID: 22781704
DOI: 10.1016/j.ejmech.2012.06.046

Abstract

We report on the design, synthesis, and in vitro evaluation of new quinoline-5,8-dione and hydroxynaphthoquinone derivatives. The synthesized compounds were evaluated for in vitro antimalarial activity against Plasmodium falciparum. Of the 15 compounds, 7a-c, 8a, 9b, 11, and 15 were effective in growth inhibition with IC(50) values of below 5 μM.

MeSH terms

Antimalarials / chemistry
Antimalarials / pharmacology
Chloroquine / pharmacology*
Drug Resistance / drug effects*
Naphthoquinones / chemistry*
Naphthoquinones / pharmacology*
Plasmodium falciparum / drug effects*
Plasmodium falciparum / growth & development
Quinolones / chemistry*
Quinolones / pharmacology*
Structure-Activity Relationship

Substances

Antimalarials
Naphthoquinones
Quinolones
Chloroquine