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Phytochemical investigations of Piper sarmentosum Roxb., yielded four compounds; three amides, identified as 3-(3’,4’,5’-trimethoxyphenylpropanoyl) pyrrolidine, 3-(4’-methoxyphenylpropanoyl) pyrrole, N -(3-phenylpropanoyl) pyrrole and a sterol namely β -sitosterol . 3-(4’-Methoxyphenylpropanoyl) pyrrole was found for the first time in this Piper species. All chemical constituents were tested for their antibacterial activity using disk diffusion method and cytotoxicity screening using sul-forhodamine B (SRB) assay. All of the compounds were found only active towards gram-positive bacteria except 3-(4’-methoxyphenylpropanoyl) pyrrole with no activity against both gram-positive and gram-negative bacteria. Meanwhile, the cytotoxicity screening using SRB assay indicated that none of these compounds was active as an anticancer agent.