Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs

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 IC50 value of 1.33 μg/mL while ciprofloxacin showed IC50 = 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.

Fluoroquinolone analogs were synthesized and screened in vitro against Plasmodium falciparum. The compound 12 was found most active with IC50 1.33 μg/mL as compared to standard ciprofloxacin with IC50 8.82 μg/mL.Figure optionsDownload as PowerPoint slideHighlights
► Novel fluoroquinolone analogs were evaluated in vitro against Plasmodium falciparum.
► The compound 12 with simple triazole showed highest activity with IC50 1.3 μg/mL.
► The standard drug antibiotic ciprofloxacin showed IC50 8.82 μg/mL.
► The compound 8 was crystallized and characterized by X-rays.
► These synthetic fluoroquinolones are more effective than ciprofloxacin.