Synthesis, Antimalarial Activity, and Structure–Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones

  • Cross R
  • Namelikonda N
  • Mutka T
 et al. 
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ICI 56,780 (5) displayed causal prophylactic and blood schizonticidal activity (ED50=0.05 mg/kg) in rodent malaria models but produced rapid acquisition of parasitological resistance in P. berghei infected mice. Herein we describe the synthesis of analogues of 5 with EC50 as low as 0.15 nM against multidrug resistant P. falciparum. Optimal activity with low cross-resistance indexes (RI) to atovaquone was achieved by introducing ortho-substituted aryl moieties at the 3-position of the 7-(2-phenoxyethoxy)-4(1H)-quinolone core.

Author-supplied keywords

  • Animals
  • Antimalarials
  • Antimalarials: chemical synthesis
  • Antimalarials: chemistry
  • Antimalarials: pharmacology
  • Atovaquone
  • Atovaquone: pharmacology
  • Cell Line
  • Drug Resistance
  • Drug Stability
  • Erythrocytes
  • Erythrocytes: drug effects
  • Erythrocytes: parasitology
  • Humans
  • Hydroxyquinolines
  • Hydroxyquinolines: chemical synthesis
  • Hydroxyquinolines: chemistry
  • Hydroxyquinolines: pharmacology
  • Liver
  • Liver: metabolism
  • Mice
  • Microsomes
  • Parasitic Sensitivity Tests
  • Permeability
  • Plasmodium falciparum
  • Plasmodium falciparum: drug effects
  • Plasmodium falciparum: isolation & purification
  • Quinolones
  • Quinolones: chemical synthesis
  • Quinolones: chemistry
  • Quinolones: pharmacology
  • Solubility
  • Stereoisomerism
  • Structure-Activity Relationship

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  • R Matthew Cross

  • Niranjan Kumar Namelikonda

  • Tina S Mutka

  • Lisa Luong

  • Dennis E Kyle

  • Roman Manetsch

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