Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs

Eur J Med Chem. 2012 May:51:52-9. doi: 10.1016/j.ejmech.2012.02.006. Epub 2012 Feb 21.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Antimalarials / toxicity
  • Cell Survival / drug effects
  • Chemistry Techniques, Synthetic
  • Fluoroquinolones / chemical synthesis*
  • Fluoroquinolones / chemistry
  • Fluoroquinolones / pharmacology*
  • Fluoroquinolones / toxicity
  • HEK293 Cells
  • Humans
  • Inhibitory Concentration 50
  • Plasmodium falciparum / drug effects*
  • Triazoles / chemistry

Substances

  • Antimalarials
  • Fluoroquinolones
  • Triazoles