In vivo study of schistosomicidal action of 1-benzyl-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one

Biomed Pharmacother. 2016 Oct:83:502-507. doi: 10.1016/j.biopha.2016.07.008. Epub 2016 Jul 18.

Abstract

Praziquantel has been the drug most widely used therapy against different forms of schistosomiasis around the world. However, this treatment has shown ineffective in humans and in experimental models of Schistosoma mansoni. New therapeutic alternatives have been tested, including the imidazolidine derivative LPSF/PT-09, which has shown high therapeutic potential in vitro. In this work, we tested the schistosomal activity of this derivative in doses of 250mg/kg and 200mg/kg in mice experimentally infected with a high parasite load of S. mansoni. Parasitological evaluations related to the number of S. mansoni worms and their oviposition were performed during the acute phase of the disease and have demonstrated moderate effectiveness of 30-54,4%. However, LPSF/PT-09 did not influence oviposition of the parasites or the embryonic development of the eggs. The results obtained in this model showed that the imidazolidine derivative LPSF/PT-09 presented significant antischistosomal activity in vivo, posing as a potential candidate for this class of drugs. However, a better understanding of the pharmacokinetics and pharmacodynamics of the imidazolidine derivative LPSF/PT-09 is needed.

Keywords: Chemotherapy; Imidazolidines; Schistosomiasis.

MeSH terms

  • Animals
  • Collagen / metabolism
  • Hydrazones / chemistry
  • Hydrazones / pharmacology*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Intestines / drug effects
  • Intestines / parasitology
  • Liver / drug effects
  • Liver / parasitology
  • Male
  • Mice
  • Ovum / drug effects
  • Schistosoma mansoni / drug effects
  • Schistosomiasis mansoni / drug therapy
  • Schistosomiasis mansoni / parasitology
  • Schistosomicides / chemistry
  • Schistosomicides / pharmacology*
  • Thiohydantoins / chemistry
  • Thiohydantoins / pharmacology*

Substances

  • 1-benzyl-4-((4-fluorophenyl)hydrazono)-5-thioxoimidazolidin-2-one
  • Hydrazones
  • Imidazoles
  • Schistosomicides
  • Thiohydantoins
  • Collagen