Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles

dc.creatorSantiago, Edna de Farias
dc.creatorOliveira, Sheilla Andrade de
dc.creatorOliveira Filho, Gevânio Bezerra de
dc.creatorMoreira, Diogo Rodrigo Magalhaes
dc.creatorGomes, Paulo André Teixeira
dc.creatorSilva, Anekécia Lauro da
dc.creatorBarros, Andréia Ferreira de
dc.creatorSilva, Aline Caroline da
dc.creatorSantos, Thiago André Ramos dos
dc.creatorPereira, Valéria Rêgo Alves
dc.creatorGonçalves, Gabriel Gazzoni Araújo
dc.creatorBrayner, Fábio André
dc.creatorAlves, Luiz Carlos
dc.creatorWanderley, Almir Gonçalves
dc.creatorLeite, Ana Cristina Lima
dc.date2018-04-03T14:24:14Z
dc.date2018-04-03T14:24:14Z
dc.date2014
dc.date.accessioned2023-09-26T20:52:10Z
dc.date.available2023-09-26T20:52:10Z
dc.identifierSANTIAGO, E. F. et al. Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles. Antimicrobial Agents and Chemotherapy, v. 58, n. 1, p. 352–363, 2014.
dc.identifier0066-4804
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/25583
dc.identifier10.1128/AAC.01900-13
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8865309
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CPNq) and Fundação Oswaldo Cruz (FIOCRUZ). FAPESB postdoctoral scholarship.
dc.descriptionSchistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-α), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials.
dc.formatapplication/pdf
dc.languageeng
dc.publisherAmerican Society for Microbiology
dc.rightsopen access
dc.subjectSchistosoma mansoni
dc.subjectEsquistossomicidas
dc.subjectPraziquantel
dc.subjectTiazóis
dc.subjectQuimioterapia
dc.subjectDroga
dc.subjectSchistosoma mansoni
dc.subjectSchistosomicides
dc.subjectPraziquantel
dc.subjectThiazoles
dc.subjectChemotherapy
dc.subjectDrugs
dc.titleEvaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles
dc.typeArticle


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