Abstract: Twelve o-hydroxybenzyl-amino acids were synthesized.Salicylaldehyde and its two-derivatives were respectively condensed with each of 4 L-α-amino acids in the presence of sodium hydroxide to obtain amino acid Schiff bases,which were subsequently reduced by NaBH₄ to produce o-hydroxy-benzyl-amino acids(3).The structures of the products were confirmed by IR,¹H NMR and elemental analysis.The result of preliminary bioassay shows that these compounds are highly effective in S.aureus inhibition at 0.05%(mass concentration) with an inhibitory ratio of 100% and have antibacterial activities to M.albicans and E.coli to some extent.Structure of the substituent R has important effect on the antibacterial activity of o-hydroxy-benzyl-amino acids.The effects of different alkyl R on antibacterial activities to M.albicans and E.coli show the following order CH(CH₃)₂>CH₃,CH₂CH(CH₃)₂>H.The bromine atoms on the benzene ring of the title compounds have little effect on antibacterial activities to M.albicans and E.coli.