Abstract BACKGROUND: A dichloromethane‐methanol extract of the seeds of Piper tuberculatum Jacq. (Piperaceae) and two isobutyl amides, 4,5‐dihydropiperlonguminine (1) and pellitorine (2), which were isolated by chromatographic methods, were assayed for their lethality against the sugarcane borer Diatraea saccharalis F. (Lepidoptera: Pyralidae). RESULTS: Bioassays were carried out with fourth‐instar caterpillars through topical application of test solutions to the dorsal surface of the prothorax, and dose–response correlations were determined. Significant insect mortalities were observed 24, 48 and 72 h after treatment at concentrations of ≥ 100 µg insect −1 . The LD 50 and LD 90 values for compound 1 were 92.83 and 176.50 µg insect −1 , and for compound 2 they were 91.19 and 184.56 µg insect −1 . CONCLUSION: According to the LD 50 and LD 90 for compounds 1 and 2, it can be inferred that the values reflect an acute lethal response to both compounds, based on interaction(s) of the toxicants with a primary target or series of targets. Thus, the amides were demonstrated to have potential value in the control of the sugarcane borer. Copyright © 2008 Society of Chemical Industry