Publications by authors named "Antônio Sérgio Alves de Almeida"

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Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents.

Rev Inst Med Trop Sao Paulo 2017 Apr 3;59:e8. Epub 2017 Apr 3.

Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.

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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http://dx.doi.org/10.1590/S1678-9946201759008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5441159PMC
April 2017
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