Piperamides and their derivatives as potential anti-trypanosomal agents

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dc.contributor.authorCotinguiba, Fernando [UNESP]
dc.contributor.authorRegasini, Luis Octavio [UNESP]
dc.contributor.authorBolzani, Vanderlan da Silva [UNESP]
dc.contributor.authorDebonsi, Hosana Maria
dc.contributor.authorPasserini, Gabriela Duo [UNESP]
dc.contributor.authorBarretto Cicarelli, Regina Maria [UNESP]
dc.contributor.authorKato, Massuo Jorge
dc.contributor.authorFurlan, Maysa [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.date.accessioned2014-05-20T14:20:15Z
dc.date.available2014-05-20T14:20:15Z
dc.date.issued2009-12-01
dc.description.abstractWe describe herein an evaluation of the trypanocidal effect of eight piperamides (1-8) isolated from Piper tuberculatum bearing dihydropyridone, piperidine, and isobutyl moieties against epimastigote forms of Trypanosoma cruzi, the causative agent of Chagas' disease. Based on such results, three hydrogenated and two hydrolyzed derivatives (10-14) were prepared and evaluated as well. The dihydropyridone amides (1-3) displayed higher anti-trypanosomal activity. The (Z)-piplartine (1) showed higher activity with a 50% inhibition concentration (IC(50)) value of 10.5 mu M, almost four times more potent than the positive control, benznidazole (IC(50) = 42.7 mu M), and should be further evaluated as a suitable hit for the design of new antiprotozoal agents.en
dc.description.affiliationUniv Estadual Paulista UNESP, Inst Quim, BR-14801970 Araraquara, SP, Brazil
dc.description.affiliationUniv São Paulo, Fac Ciencias Farmaceut, BR-14040903 Ribeirao Preto, SP, Brazil
dc.description.affiliationUniv Estadual Paulista UNESP, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUniv São Paulo, Inst Quim, BR-05508900 São Paulo, Brazil
dc.description.affiliationUnespUniv Estadual Paulista UNESP, Inst Quim, BR-14801970 Araraquara, SP, Brazil
dc.description.affiliationUnespUniv Estadual Paulista UNESP, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipIdFAPESP: 03/11524-9
dc.description.sponsorshipIdCNPq: 07/56140-4
dc.description.sponsorshipIdCNPq: 03/00886-7
dc.format.extent703-711
dc.identifierhttp://dx.doi.org/10.1007/s00044-008-9161-9
dc.identifier.citationMedicinal Chemistry Research. Cambridge: Birkhauser Boston Inc, v. 18, n. 9, p. 703-711, 2009.
dc.identifier.doi10.1007/s00044-008-9161-9
dc.identifier.issn1054-2523
dc.identifier.lattes4484083685251673
dc.identifier.lattes1308042794786872
dc.identifier.urihttp://hdl.handle.net/11449/26082
dc.identifier.wosWOS:000272617700001
dc.language.isoeng
dc.publisherBirkhauser Boston
dc.relation.ispartofMedicinal Chemistry Research
dc.relation.ispartofjcr1.607
dc.relation.ispartofsjr0,422
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectPiperamidesen
dc.subjectAnti-trypanosomalen
dc.subjectTrypanosoma cruzien
dc.subjectPiper tuberculatumen
dc.subjectPiperaceaeen
dc.titlePiperamides and their derivatives as potential anti-trypanosomal agentsen
dc.typeArtigo
dcterms.licensehttp://www.springer.com/open+access/authors+rights?SGWID=0-176704-12-683201-0
dcterms.rightsHolderBirkhauser Boston Inc
unesp.author.lattes4484083685251673
unesp.author.lattes1308042794786872
unesp.campusUniversidade Estadual Paulista (Unesp), Instituto de Química, Araraquarapt

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