title: In vivo study of schistosomicidal action of 1-benzyl-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one.
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.
authors.affiliation: 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.
authors.forename: Anekécia Lauro
authors.initials: AL
authors.lastname: da Silva
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
authors.forename: Jamerson Ferreira
authors.initials: JF
authors.lastname: de Oliveira
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
authors.forename: Willams Leal
authors.initials: WL
authors.lastname: Silva
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
authors.forename: Aracelly França
authors.initials: AF
authors.lastname: Luis
authors.affiliation: Centro de Pesquisa Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil.
authors.forename: Edna
authors.initials: E
authors.lastname: de Farias Santiago
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
authors.forename: Antônio Sérgio
authors.initials: AS
authors.lastname: Alves de Almeida Júnior
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil; Instituto Federal de Alagoas-Campus Maragogi, Maragogi, AL, 57955-000, Brazil.
authors.forename: Tiago Bento
authors.initials: TB
authors.lastname: de Oliveira
authors.affiliation: Centro de Pesquisa Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil.
authors.forename: Veruska Cíntia Alexandrino
authors.initials: VCA
authors.lastname: de Souza
authors.affiliation: Centro de Pesquisa Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil.
authors.forename: Andréia Ferreira
authors.initials: AF
authors.lastname: de Barros
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil.
authors.forename: Ivan da Rocha
authors.initials: IDR
authors.lastname: Pitta
authors.affiliation: Centro de Pesquisa Aggeu Magalhães, Fundação Oswaldo Cruz (FIOCRUZ), 50670-420 Recife, PE, Brazil.
authors.forename: Sheilla Andrade
authors.initials: SA
authors.lastname: de Oliveira
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Departamento de Antibióticos, 50670-901, Recife, PE, Brazil. Electronic address: nenalima.mariadocarmo@gmail.com.
authors.forename: Maria do Carmo
authors.initials: MDC
authors.lastname: Alves de Lima
mesh_terms: D000818:Animals; D003094:Collagen / Q000378:metabolism; D006835:Hydrazones / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D007422:Intestines / Q000187:drug effects / Q000469:parasitology; D008099:Liver / Q000187:drug effects / Q000469:parasitology; D008297:Male; D051379:Mice; D010063:Ovum / Q000187:drug effects; D012550:Schistosoma mansoni / Q000187:drug effects; D012555:Schistosomiasis mansoni / Q000188:drug therapy / Q000469:parasitology; D012556:Schistosomicides / Q000737:chemistry / Q000494:pharmacology*; D013867:Thiohydantoins / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C000613898:1-benzyl-4-((4-fluorophenyl)hydrazono)-5-thioxoimidazolidin-2-one; D006835:Hydrazones; D007093:Imidazoles; D012556:Schistosomicides; D013867:Thiohydantoins; D003094:Collagen
keywords: Chemotherapy; Imidazolidines; Schistosomiasis