A simple total synthesis of naturally occurring magnolamide, N-[4-(2-formyl-5-hydroxymethylpyrrol-1-yl)butyl]-3-(4-hydroxy-3-methoxyphenyl)-2-propenamide, from pyrrole-2,5-dicarbaldehyde was performed in six steps and its antioxidant activity was compared with probucol and resveratrol. Results showed that magnolamide markedly inhibited CuSO4-induced oxidation of human low-density lipoprotein (IC50 = 9.7 μ M) with similar activity to probucol and resveratrol.