title: Antischistosomal action of thioxo-imidazolidine compounds: an ultrastructural and cytotoxicity study.
abstract: Schistosomiasis is a disease caused by helminthes of the genus Schistosoma, which threatens approximately 207 million people worldwide. Recently, strains of Schistosoma mansoni appear to be developing tolerance and resistance against Praziquantel, the most commonly available drug on the market used in the treatment of disease. This worrisome development justifies studies that seek alternatives for the prevention, treatment and cure of this disease. This study aimed to evaluate the in vitro activity of new imidazolidine compounds 1-benzyl-4-[(4-chloro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-5) and 1-(4-chloro-benzyl)-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-11) against adult worms of S. mansoni. LPSF/PT-5 and LPSF/PT-11 imidazolidine derivatives showed relevant schistosomicidal activity in vitro and induced significant ultrastructural alterations in worms and cell death: results similar to praziquantel. Thus, it is possible that these imidazolidine derivatives can be future candidates as schistosomotic drugs, but further studies are needed to elucidate the induced mechanisms behind this response.
authors.affiliation: Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Centro de Ciências Biológicas, Universidade Federal de Pernambuco (UFPE), Av. Prof. Moraes Rego s/n, Cidade Universitária, Recife, PE, Brazil. lemoineju@gmail.com
authors.forename: Juliana Kelle A L
authors.initials: JK
authors.lastname: Neves
authors.forename: Maria do Carmo Alves
authors.initials: Mdo C
authors.lastname: de Lima
authors.forename: Valéria Rego Alves
authors.initials: VR
authors.lastname: Pereira
authors.forename: Cristiane Moutinho Lagos
authors.initials: CM
authors.lastname: de Melo
authors.forename: Christina Alves
authors.initials: CA
authors.lastname: Peixoto
authors.forename: Ivan da Rocha
authors.initials: Ida R
authors.lastname: Pitta
authors.forename: Mônica Camelo Pessoa Azevedo
authors.initials: MC
authors.lastname: Albuquerque
authors.forename: Suely Lins
authors.initials: SL
authors.lastname: Galdino
mesh_terms: D000818:Animals; D017304:Annexin A5 / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects; D001700:Biomphalaria; D002470:Cell Survival / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry; D005260:Female; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry; D048289:Imidazolidines / Q000494:pharmacology* / Q000633:toxicity; D007202:Indicators and Reagents / Q000737:chemistry; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008855:Microscopy, Electron, Scanning; D009336:Necrosis; D011223:Praziquantel / Q000494:pharmacology / Q000633:toxicity; D011419:Propidium / Q000737:chemistry; D012550:Schistosoma mansoni / Q000187:drug effects* / Q000648:ultrastructure; D012555:Schistosomiasis mansoni / Q000188:drug therapy / Q000469:parasitology*; D012556:Schistosomicides / Q000494:pharmacology* / Q000633:toxicity; D013154:Spleen / Q000166:cytology / Q000187:drug effects / Q000473:pathology
chemical_list: D017304:Annexin A5; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D048289:Imidazolidines; D007202:Indicators and Reagents; D012556:Schistosomicides; D011419:Propidium; D011223:Praziquantel; D016650:Fluorescein-5-isothiocyanate