Sesamol, one of constituents isolated from sesame seed (Sesamum indicum L.) has been known to have natural antioxidant property. Nicotinic acid and clofibric acid have been used for treatment of hyperlipidemia. Sesamol derivatives prepared by conjugation with nicotinic acid (SJ-301) and clofibric acid (SJ-302) were expected to have various biological activity caused by synergistic effect of sesamol. Thus, this study were carried out to investigate the synthesis of sesamol derivatives from seasamol and antihyperlipidemia drugs and their biological activities. As a result, SJ-301 showed a stronger antihyperlipidemia activity in vivo and inhibitory effect on $TNF-{alpha}$ release in vitro compared to the original agents such as sesamol, nicotinic acid and clofibric acid.