dc.creatorSilva, Luana Maria Mariz Gomes da
dc.creatorOliveira, Jamerson Ferreira de
dc.creatorSilva, Willams Leal
dc.creatorSilva, Anekecia Lauro da
dc.creatorAlmeida Junior, Antônio Sérgio Alves de
dc.creatorSantos, Victor Hugo Barbosa dos
dc.creatorAlves, Luiz Carlos
dc.creatorSantos, Fábio André Brayner dos
dc.creatorCosta, Vlaudia Maria Assis
dc.creatorAires, André de Lima
dc.creatorLima, Maria do Carmo Alves de
dc.creatorAlbuquerque, Monica Camelo Pessoa de Azevedo
dc.date2019-05-16T15:56:41Z
dc.date2019-05-16T15:56:41Z
dc.date2018
dc.date.accessioned2023-09-26T23:23:13Z
dc.date.available2023-09-26T23:23:13Z
dc.identifierSILVA, Luana Maria Mariz Gomes da et al. New 1,3-benzodioxole derivatives: Synthesis, evaluation of in vitro schistosomicidal activity and ultrastructural analysis. Chemico-Biological Interactions, v. 283, p. 20-29, Mar. 2018.
dc.identifier1872-7786
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/33115
dc.identifier10.1016/j.cbi.2018.01.016
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8890012
dc.descriptionSchistosomiasis is considered a serious public health problem in 78 countries and territories located in Africa, Asia and America and it is estimated in more than 249 million people infected by any of the species of Schistosoma. The exclusive use of praziquantel (PZQ), effective drug against all species of Schistosoma, has been the basis of the development of a possible resistance against the strains of this parasite. In addition, PZQ is not effective against young forms of worms. Thus, there is a need for the development of new drugs with schistosomicidal activity. The objective of this work was to synthesize and to evaluate the therapeutic potential of new benzodioxole derivatives (3-14) candidates for schistosomicidal drugs. All compounds synthesized showed in vitro schistosomicidal activity. The derivative 12 was considered the best compound, since it took 100% of worms to mortality in the first 72 h of exposure at the concentration of 100 μM and 83.3% at the concentration of 50 μM. Furthermore, male and female adult worms, incubated for 24 h with the compound 12 showed tegument damages characterized by extensive desquamation and edema, tuber destruction, bubble formation and exposure of the muscle layer. This compound has a restricted structure, where the thiazolidinone is attached to the 4-position of the 1,3-benzodioxol ring. The structural conformation of derivative 12 was probably responsible for the promising schistosomicidal activity, where the presence of an electron/conformational restriction of the thiazolidine ring, as well as the action of bromine as a bulk substitute, favored an increase in biological activity. In addition, tegumentary changes caused by derivative 12 may also have been responsible for the death of adult worms of Schistosoma mansoni. Therefore, we verified that the results obtained in this study make benzodioxole derivatives possible candidates for prototypes of new schistosomicidal drugs.
dc.description2050-01-01
dc.formatapplication/pdf
dc.languageeng
dc.rightsrestricted access
dc.subjectBenzodioxole
dc.subjectSchistosomicidal activity
dc.subjectSchistosoma mansoni
dc.subjectScanning electron microscopy
dc.subjectAnimais
dc.subjectSobrevivência Celular / efeitos de drogas
dc.subjectDioxoles / química
dc.subjectDioxoles / farmacologia
dc.subjectDioxoles / uso terapêutico
dc.subjectCélulas HeLa
dc.subjectHumanos
dc.subjectMicroscopia, elétron, varredura
dc.subjectPraziquantel / farmacologia
dc.subjectPraziquantel / uso terapêutico
dc.subjectSchistosoma mansoni / efeitos de drogas
dc.subjectSchistosoma mansoni / ultraestrutura
dc.subjectEsquistossomose / quimioterapia
dc.subjectEsquistossomose / patologia
dc.subjectEsquistossomicidas / síntese química
dc.subjectEsquistossomicidas / farmacologia
dc.subjectEsquistossomicidas / uso terapêutico
dc.titleNew 1,3-benzodioxole derivatives: Synthesis, evaluation of in vitro schistosomicidal activity and ultrastructural analysis
dc.typeArticle


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