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Please use this identifier to cite or link to this item: http://acervodigital.unesp.br/handle/11449/76337
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dc.contributor.authorBlau, Lorena-
dc.contributor.authorMenegon, Renato Farina-
dc.contributor.authorTrossini, Gustavo H. G.-
dc.contributor.authorMolino, João Vitor Dutra-
dc.contributor.authorVital, Drielli Gomes-
dc.contributor.authorCicarelli, Regina Maria Barretto-
dc.contributor.authorPasserini, Gabriela Duó-
dc.contributor.authorBosquesi, Priscila Longhin-
dc.contributor.authorChin, Chung Man-
dc.date.accessioned2014-05-27T11:30:16Z-
dc.date.accessioned2016-10-25T18:52:59Z-
dc.date.available2014-05-27T11:30:16Z-
dc.date.available2016-10-25T18:52:59Z-
dc.date.issued2013-08-27-
dc.identifierhttp://dx.doi.org/10.1016/j.ejmech.2013.04.022-
dc.identifier.citationEuropean Journal of Medicinal Chemistry, v. 67, p. 142-151.-
dc.identifier.issn0223-5234-
dc.identifier.issn1768-3254-
dc.identifier.urihttp://hdl.handle.net/11449/76337-
dc.identifier.urihttp://acervodigital.unesp.br/handle/11449/76337-
dc.description.abstractThe present work reports on the synthesis, biological assaying and docking studies of a series of 12 aryl thiosemicarbazones, which were planned to act over two main enzymes, cruzain and trypanothione reductase. These enzymes are used as targets of trypanocidal activity in Chagas disease control with a minimal mutagenic profile. Three p-nitroaromatic thiosemicarbazones showed high activity against Trypanosoma cruzi in in vitro assays (IC50 < 57 μM), and no mutagenic profile was observed in micronucleous tests. Although the in vitro inhibition test showed that 10-μM doses of eight compounds inhibited cruzain activity, no correlation was found between cruzain inhibition and trypanocidal activity. © 2013 Elsevier Masson SAS. All rights reserved.en
dc.format.extent142-151-
dc.language.isoeng-
dc.sourceScopus-
dc.subjectChagas disease-
dc.subjectCruzain-
dc.subjectDocking-
dc.subjectMutagenicity-
dc.subjectOxidative stress-
dc.subjectThiosemicarbazone-
dc.subject2 amino 1 (3 nitrophenyl)ethan 1 one thiosemicarbazone-
dc.subject2 amino 1 (4 nitro) acetophenone thiosemicarbazone hemisuccinate amide-
dc.subject2 amino 1 (4 nitro)acetophenone thiosemicarbazone-
dc.subject2 amino 1 phenylethan 1 one thiosemicarbazone-
dc.subject2 hidroxy 1 (4 nitro) acetophenone thiosemicarbazone hemisuccinate ester-
dc.subject2 hydroxy 1 (4 nitro)acetophenone thiosemicarbazone-
dc.subject3 amino 4 nitroacetophenone thiosemicarbazone-
dc.subject3 nitro 4 aminoacetophenone thiosemicarbazone-
dc.subject4 aminoacetophenone thiosemicarbazone-
dc.subjectacetophenone thiosemicarbazone-
dc.subjectaminoacetophenone thiosemicarbazone-
dc.subjectantiprotozoal agent-
dc.subjectcruzipain-
dc.subjectthiosemicarbazone derivative-
dc.subjecttrypanothione reductase-
dc.subjectunclassified drug-
dc.subjectantiprotozoal activity-
dc.subjectbiological activity-
dc.subjectbromination-
dc.subjectconcentration response-
dc.subjectdrug design-
dc.subjectdrug mechanism-
dc.subjectdrug structure-
dc.subjectdrug synthesis-
dc.subjectIC 50-
dc.subjectin vitro study-
dc.subjectmelting point-
dc.subjectmolecular docking-
dc.subjectmutagenic activity-
dc.subjectmutagenicity-
dc.subjectnonhuman-
dc.subjecttrypanocidal activity-
dc.subjectTrypanosoma cruzi-
dc.titleDesign, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidatesen
dc.typeoutro-
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)-
dc.contributor.institutionUniversidade do Vale do Paraíba-
dc.contributor.institutionUniversidade de São Paulo (USP)-
dc.description.affiliationDepartamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista, Rodovia Araraquara-Jaú Km 01, 14801-902 Araraquara, SP-
dc.description.affiliationInstituto de Pesquisa e Desenvolvimento Universidade do Vale do Paraíba, Avenida Shishima Hifume 2911, 12244-000 São José dos Campos, SP-
dc.description.affiliationDepartamento de Farmácia Faculdade de Ciências Farmacêuticas Universidade de São Paulo, Professor Lineu Prestes 580, 05508-900 São Paulo, SP-
dc.description.affiliationDepartamento de Ciências Biológicas Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista, Rodovia Araraquara-Jaú Km 01, 14801-902 Araraquara, SP-
dc.description.affiliationUnespDepartamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista, Rodovia Araraquara-Jaú Km 01, 14801-902 Araraquara, SP-
dc.description.affiliationUnespDepartamento de Ciências Biológicas Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista, Rodovia Araraquara-Jaú Km 01, 14801-902 Araraquara, SP-
dc.identifier.doi10.1016/j.ejmech.2013.04.022-
dc.identifier.wosWOS:000325121800016-
dc.rights.accessRightsAcesso restrito-
dc.relation.ispartofEuropean Journal of Medicinal Chemistry-
dc.identifier.scopus2-s2.0-84882528324-
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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