Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs

Abstract

Fluoroquinolone analogs were synthesized by simple alkylation followed by click chemistry and evaluated for their antimalarial in vitro against chloroquine sensitive strain of Plasmodium falciparum while ciprofloxacin was used as standard. Our results showed that the compound 12 was found most active with IC 50 value of 1.33 μg/mL while ciprofloxacin showed IC 50 = 8.81 μg/mL. Therefore, screening of either known or unknown quinolone/fluoroquinolone analogs are worthwhile to find more potent antimalarial drugs which might prove useful in the treatment of mild or severe malaria in human either alone or in combination with existing antimalarial drugs. © 2012 Elsevier Masson SAS. All rights reserved.