Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni

Parasitol Res. 2010 Aug;107(3):531-8. doi: 10.1007/s00436-010-1886-y. Epub 2010 May 4.

Abstract

The only drug available for treating schistosomiasis is praziquantel, however there are already reports of resistance to its use in treatment, making it necessary to search and develop new compounds to combat schistosomiasis. We tested, in vitro, two new products, Laboratório de Planejamento de Síntese de Fármacos (LPSF)/5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one (RZS-2) and LPSF/5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one (RZS-5) imidazolidines, against adult worms of Schistosoma mansoni. Efficacy and safety of these compounds were analyzed through IC50 cytotoxicity, immune response and cell viability tests. At different concentrations ranging from 40-640 microM, the imidazolidines produced motor abnormalities, inhibition of pairing and oviposition and mortality within 24 h at the higher concentrations. Although not triggering changes in IFN-gamma and IL-10, LPSF/RZS-2 and LPSF/RZS-5 induced production of nitric oxide and showed similar behavior to praziquantel in the cell death test.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Imidazolidines / administration & dosage
  • Imidazolidines / immunology
  • Imidazolidines / pharmacology*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Parasitic Sensitivity Tests
  • Schistosoma mansoni / drug effects*
  • Schistosomiasis mansoni / drug therapy
  • Schistosomiasis mansoni / parasitology
  • Schistosomicides / administration & dosage
  • Schistosomicides / immunology
  • Schistosomicides / pharmacology*

Substances

  • 5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one)
  • 5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one)
  • Imidazolidines
  • Schistosomicides