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Rev. Inst. Med. Trop. Säo Paulo ; 59: e8, 2017. tab, graf
Article Dans Anglais | LILACS | ID: biblio-842798

Résumé

ABSTRACT Introduction: Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives. Material and methods: We synthesized two novel imidazolidine derivatives: (LPSF/PTS10) (Z)-1-(2-chloro-6-fluorobenzyl)-4-(4-dimethylaminobenzylidene)-5-thioxoimidazolidin-2-one and (LPSF/PTS23) (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one. The structures of two compounds were determined by spectroscopic methods. During the biological assays, parameters such as motility, oviposition, mortality and analysis by Scanning Electron Microscopy were performed. Results: LPSF/PTS10 and LPSF/PTS23 were considered to be active in the separation of coupled pairs, mortality and to decrease the motor activity. In addition, LPSF/PTS23 induced ultrastructural alterations in worms, after 24 h of contact, causing extensive erosion over the entire body of the worms. Conclusion: The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.


Sujets)
Humains , Animaux , Souris , Imidazolidines/pharmacologie , Cellules souches du sang périphérique/effets des médicaments et des substances chimiques , Schistosoma mansoni/effets des médicaments et des substances chimiques , Schistosomicides/pharmacologie , Imidazolidines/synthèse chimique , Imidazolidines/toxicité , Microscopie électronique à balayage , Tests de sensibilité parasitaire , Schistosoma mansoni/ultrastructure , Schistosomicides/synthèse chimique , Schistosomicides/toxicité , Facteurs temps
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