Glycine ethyl ester hydrochloride, L-Alanine ethyl ester hydrochloride, L-leucine ethyl ester hydrochloride, L-methionine methyl ester hydrochloride and L-tyrosine methyl ester hydrochloride were used to react with oleic acid in presence of EDC/HOBt to produce five kinds of amino acid derivatives of oleic acid. In addition, glycine ethyl ester hydrochloride and L-alanine ethyl ester hydrochloride were reacted with dodecanedioic acid to produce two amino acid derivatives of dodecanedioic acid. The results showed that seven products were synthesized with yields higher than 75%. The structures of the products were characterized by FTIR, TGA, 1HNMR and LC-MS. The dispersibilities of the products were tested, and the antibacterial activities of the products against Staphylococcus aureus and Escherichia coli were investigated. The results showed that the products were capable of dispersing in both aqueous and organic phases. Moreover, these fatty acid acyl amino acid esters showed obvious antimicrobial activities. The oleoyl leucine ethyl ester can effectively inhibit the growth of Staphylococcus aureus (the number of bacteria is decreased from 2×109 CFU/mL to 1.4×107 CFU/mL). The oleoyl tyrosine methyl ester can inhibit Escherichia coli (the number of bacteria is decreased from 2×109 CFU/mL to 1.8×107 CFU/mL).