Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
Rev. Inst. Med. Trop. Säo Paulo
;
59: e8, 2017. tab, graf
Artigo
em Inglês
| LILACS
| ID: biblio-842798
ABSTRACT
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.
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Assunto principal:
Schistosoma mansoni
/
Esquistossomicidas
/
Imidazolidinas
/
Células-Tronco de Sangue Periférico
Limite:
Animais
/
Humanos
Idioma:
Inglês
Revista:
Rev. Inst. Med. Trop. Säo Paulo
Assunto da revista:
Medicina Tropical
Ano de publicação:
2017
Tipo de documento:
Artigo
País de afiliação:
Brasil
Instituição/País de afiliação:
Fundação Oswaldo Cruz/BR
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