A peptide coupling reaction between 1-(R)-phenylethylalanine and cinnamic acid derivatives has been successfully employed for the synthesis of a set of small molecules. The antimalarial activity of these derivative molecules is reported. The compounds have been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of P. falciparum as well as their cytotoxic activity against HUVEC cells. For 3D7, the most active molecule was compound 8 with IC50 of 23.6 nM/mL comparable to that of chloroquine (18.5 nM/mL). The products were characterized by IR, NMR and MS analysis.