Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model

J Med Chem. 2006 Jul 27;49(15):4795-8. doi: 10.1021/jm0606241.

Abstract

Several aza-fused rhodacyanines were synthesized and assessed for their in vitro and in vivo antimalarial activities against Plasmodium falciparum K1 and P. berghei. All synthetic compounds showed strong selective antimalarial in vitro activity. Class II azarhodacyanines, 3, consisting of four heterocyclic units, were found to display good parasitemia suppression and low acute toxicity in vivo. Among them, 3c appeared to be the most effective at a dose of 20-25 mg kg(-1) day(-1) (ip).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology
  • Antimalarials / toxicity
  • Aza Compounds / chemical synthesis*
  • Aza Compounds / pharmacology
  • Aza Compounds / toxicity
  • Cell Line
  • Drug Resistance
  • Malaria / drug therapy*
  • Mice
  • Plasmodium berghei / drug effects*
  • Plasmodium falciparum / drug effects
  • Pyridinium Compounds / chemical synthesis*
  • Pyridinium Compounds / pharmacology
  • Pyridinium Compounds / toxicity
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology
  • Thiazoles / toxicity

Substances

  • Antimalarials
  • Aza Compounds
  • Pyridinium Compounds
  • Thiazoles
  • rhodacyanine