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

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

Author information

1
Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil; Universidade Federal do Vale do São Francisco (UNIVASF), Departamento de Medicina, 48607-190, Paulo Afonso, BA, Brazil.
2
Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
3
Centro de Pesquisa Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil.
4
Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil; Instituto Federal de Alagoas-Campus Maragogi, Maragogi, AL, 57955-000, Brazil.
5
Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil. Electronic address: nenalima.mariadocarmo@gmail.com.

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

PMID:
27434866
DOI:
10.1016/j.biopha.2016.07.008
[Indexed for MEDLINE]

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