Abstract: N-phenylpropenoyl-L-amino acids(NPAs) are phenylpropenoyled products of amino acids with multiple pharmacological activities, such as anti-oxidative, anti-microbial, tyrosinase-inhibiting, α-glucosidase-inhibiting, and anti-neuroinflammatory activities. NPAs have very promising application prospect in the fields of medicine, food and cosmetics. This paper reviewed recent advances in synthetic methods and pharmacological activities of NPAs, so as to provide references for further study of their structure-activity relationship and development of NPAs.