Cotinguiba, Fernando [UNESP]Regasini, Luis Octavio [UNESP]Bolzani, Vanderlan da Silva [UNESP]Debonsi, Hosana MariaPasserini, Gabriela Duo [UNESP]Barretto Cicarelli, Regina Maria [UNESP]Kato, Massuo JorgeFurlan, Maysa [UNESP]2014-05-202014-05-202009-12-01Medicinal Chemistry Research. Cambridge: Birkhauser Boston Inc, v. 18, n. 9, p. 703-711, 2009.1054-2523http://hdl.handle.net/11449/26082We 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.703-711engPiperamidesAnti-trypanosomalTrypanosoma cruziPiper tuberculatumPiperaceaeArtigo10.1007/s00044-008-9161-9WOS:000272617700001Acesso restrito44840836852516731308042794786872