title: Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni.
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.
authors.affiliation: Laboratório de Planejamento e Síntese de Fármacos (LPSF) do Departamento de Antibióticos-UFPE, Recife, Pernambuco, Brazil. lemoineju@gmail.com
authors.forename: Juliana Kelle de Andrade Lemoine
authors.initials: JK
authors.lastname: Neves
authors.forename: Sandra Paula Sarinho
authors.initials: SP
authors.lastname: Botelho
authors.forename: Cristiane Moutinho Lagos
authors.initials: CM
authors.lastname: de Melo
authors.forename: Valéria Rêgo Alves
authors.initials: VR
authors.lastname: Pereira
authors.forename: Maria do Carmo Alves
authors.initials: Mdo C
authors.lastname: de Lima
authors.forename: Ivan da Rocha
authors.initials: Ida R
authors.lastname: Pitta
authors.forename: Mônica Camelo Pessoa de Azevedo
authors.initials: MC
authors.lastname: Albuquerque
authors.forename: Suely Lins
authors.initials: SL
authors.lastname: Galdino
mesh_terms: D000818:Animals; D005260:Female; D048289:Imidazolidines / Q000008:administration & dosage / Q000276:immunology / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D021261:Parasitic Sensitivity Tests; D012550:Schistosoma mansoni / Q000187:drug effects*; D012555:Schistosomiasis mansoni / Q000188:drug therapy / Q000469:parasitology; D012556:Schistosomicides / Q000008:administration & dosage / Q000276:immunology / Q000494:pharmacology*
chemical_list: C553638:5-(4-chloro-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one); C553639:5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one); D048289:Imidazolidines; D012556:Schistosomicides