Antiplasmodial and leishmanicidal activities of 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives

Molecules. 2012 Aug 7;17(8):9451-61. doi: 10.3390/molecules17089451.

Abstract

Malaria and leishmaniasis are two of the World's most important tropical parasitic diseases. Thirteen new 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives (CPCQs) were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against erythrocytic forms of Plasmodium falciparum and axenic forms of Leishmania infantum. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. None of the tested compounds was efficient against Plasmodium, but two of them showed good activity against Leishmania. Toxicity on VERO was correlated with leishmanicidal properties.

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / pharmacology*
  • Catalysis
  • Chlorocebus aethiops
  • Dimethylformamide / chemistry
  • Drug Evaluation, Preclinical
  • Ethylamines / chemistry
  • Inhibitory Concentration 50
  • Leishmania infantum / drug effects*
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology*
  • Plasmodium falciparum / drug effects*
  • Quinoxalines / chemical synthesis
  • Quinoxalines / pharmacology*
  • Solvents / chemistry
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Antiprotozoal Agents
  • Ethylamines
  • Piperazines
  • Quinoxalines
  • Solvents
  • Dimethylformamide
  • triethylamine