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We 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 (IC₅₀) value of 10.5 μM, almost four times more potent than the positive control, benznidazole (IC₅₀ = 42.7 μM), and should be further evaluated as a suitable hit for the design of new antiprotozoal agents.