Melanin is a dark pigment produced by melanocytes in the stratum basal of the epidermis. Although melanin is synthesized as a natural photo-protectant, the accumulation of abnormally produced melanin leads to a serious aesthetic problem. In melanin synthetic pathway, tyrosinase is a key enzyme which catalyzes ortho-hydroxylation of L-tyrosine and oxidation of L-DOPA in the early stage of melanogenesis. Thus, tyrosinase is a major target in the cosmetic industry. Recently, the study on inhibition of tyrosinase activity has drawn attention because it has been reported that it can generate cancer and neurodegenerative diseases such as Parkinson’s disease. Hydroxamic acid is a well-known metal chelator and has been intensively investigated due to a wide range of biological activities. However, its tyrosinase inhibitory activity or effects on melanogenesis was rarely reported. In this study, we synthesized L-amino acid-hydroxamic acid derivatives of bio active compounds and measured its tyrosinase inhibitory activity.