Species of Piper genus are known for their numerous biological activities and their diverse phytochemical composition. The object of this work was to evaluate the antibacterial activity of extracts obtained from seven Piperaceae species. Broth microdilution technique was used for biological evaluation and some phytochemical nuclei present in the bioactive extracts were identified by thin layer chromatography and characterization reactions. Among the most important results, it is highlighted the inhibitory effect of the methanolic extract from Piper pesaresanum against Methicillin-resistant Staphylococcus aureus ATTC 43300, with minimum inhibitory concentration of 62.5 μg/mL. Additionally, secondary metabolites such as alkaloids, phenols and flavonoids were detected in this extract. In conclussion, the species P. pesaresanum showed high potential for bioguided search of antibacterial compounds against multidrug resistant S. aureus.