New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain.
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.
Department of Chemistry, University of Paderborn, Warburger Strasse 100, 33098 Paderborn, Germany. Hidayat110@gmail.com
Hidayat
H
Hussain
Sabine
S
Specht
Salem R
SR
Sarite
Achim
A
Hoerauf
Karsten
K
Krohn
D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology*; D004351:Drug Resistance / Q000187:drug effects*; D009285:Naphthoquinones / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D015363:Quinolones / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000962:Antimalarials; D009285:Naphthoquinones; D015363:Quinolones; D002738:Chloroquine