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Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates

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dc.contributor.authorBlau, Lorena [UNESP]
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 [UNESP]
dc.contributor.authorPasserini, Gabriela Duó [UNESP]
dc.contributor.authorBosquesi, Priscila Longhin [UNESP]
dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade do Vale do Paraíba
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.date.accessioned2014-05-27T11:30:16Z
dc.date.available2014-05-27T11:30:16Z
dc.date.issued2013-08-27
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.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.format.extent142-151
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.doi10.1016/j.ejmech.2013.04.022
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.scopus2-s2.0-84882528324
dc.identifier.urihttp://hdl.handle.net/11449/76337
dc.identifier.wosWOS:000325121800016
dc.language.isoeng
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.ispartofjcr4.816
dc.relation.ispartofsjr1,266
dc.rights.accessRightsAcesso restritopt
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.typeArtigopt
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dspace.entity.typePublication
relation.isDepartmentOfPublication5004bcab-94af-4939-b980-091ae9d0a19e
relation.isDepartmentOfPublicatione214da1b-9929-4ae9-b8fd-655e9bfeda4b
relation.isDepartmentOfPublication.latestForDiscovery5004bcab-94af-4939-b980-091ae9d0a19e
relation.isOrgUnitOfPublication95697b0b-8977-4af6-88d5-c29c80b5ee92
relation.isOrgUnitOfPublication.latestForDiscovery95697b0b-8977-4af6-88d5-c29c80b5ee92
unesp.author.lattes9734333607975413[9]
unesp.author.orcid0000-0003-2475-9807[4]
unesp.author.orcid0000-0003-3634-2531[3]
unesp.author.orcid0000-0001-9270-0466[5]
unesp.author.orcid0000-0003-4141-0455[9]
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentCiências Biológicas - FCFpt
unesp.departmentFármacos e Medicamentos - FCFpt

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