dc.contributorUniversidade Estadual Paulista (UNESP)
dc.creatorCotinguiba, Fernando
dc.creatorRegasini, Luis Octavio
dc.creatorBolzani, Vanderlan da Silva
dc.creatorDebonsi, Hosana Maria
dc.creatorPasserini, Gabriela Duo
dc.creatorBarretto Cicarelli, Regina Maria
dc.creatorKato, Massuo Jorge
dc.creatorFurlan, Maysa
dc.date2014-05-20T14:20:15Z
dc.date2016-10-25T17:41:31Z
dc.date2014-05-20T14:20:15Z
dc.date2016-10-25T17:41:31Z
dc.date2009-12-01
dc.date.accessioned2017-04-05T22:33:42Z
dc.date.available2017-04-05T22:33:42Z
dc.identifierMedicinal Chemistry Research. Cambridge: Birkhauser Boston Inc, v. 18, n. 9, p. 703-711, 2009.
dc.identifier1054-2523
dc.identifierhttp://hdl.handle.net/11449/26082
dc.identifierhttp://acervodigital.unesp.br/handle/11449/26082
dc.identifier10.1007/s00044-008-9161-9
dc.identifierWOS:000272617700001
dc.identifierhttp://dx.doi.org/10.1007/s00044-008-9161-9
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/870901
dc.descriptionWe 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.
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.languageeng
dc.publisherBirkhauser Boston
dc.relationMedicinal Chemistry Research
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectPiperamides
dc.subjectAnti-trypanosomal
dc.subjectTrypanosoma cruzi
dc.subjectPiper tuberculatum
dc.subjectPiperaceae
dc.titlePiperamides and their derivatives as potential anti-trypanosomal agents
dc.typeOtro


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