Résumé : Basing on the previous syntheses of ester compounds containing gramine functional groups, the researchers synthesized two novel acylamino compounds containing gramine groups and the structures of target compound were established using 1HNMR, 13CNMR, IR spectra, and elemental analysis. The antibacterial activity of the synthesized compounds against Escherichia coli and Staphylococcus aureus, as well as their antifouling activity were studied. The results showed that these compounds possessed high antibacterial activity and a minimal inhibitory concentration value of 0.03 mg/mL against bacteria. Moreover, their antifouling properties are superior to cuprous oxide and chlorothalonil, which are widely used as antifoulants. Furthermore, quantitative structure activity relationship studies with antibacterial activity of the nine gramine compounds were established. These provide theoretical and technical bases for preparing environment-friendly antifouling coatings with the compounds as antifouling agents.