The rupestonic acid (compound 1) was isolated from the Chinese herbal medicine Artemisia rupestris L. (its Chinese name being Yizhihao). Then, 13 rupestonic acid amide derivatives 2a similar to 2m were synthesized using rupestonic acid and organic amines in the presence of DCC, HOBt/DMAP and their structures were comfirmed by the methods of IR, (1)HNMR, and ESI-MS. All compounds were preliminarily assayed in vitro against influenza A(3), B, herpes simplex I (HSV-I) and herpes simplex II (HSV-II) viruses, showing that 2a was inhibitive to both influenza A(3) and B viruses, and had the higher inhibition against influenza B virus than the parent compound 1. The inhibition of 2d against influenza B virus was 16-fold higher than that of the parent compound and 2e was more active both to HSV-I and HSV-II viruses