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Anthranilic acid derivatives (3-5) containing the long chain components of N-stearoyl, -oleoyl, and -linoleoyl groups were synthesized for the study of prolyl endopeptidase (PEP, EC 3.4.21.26) inhibitory activity. Compounds 3-5 showed competitive PEP inhibition with IC50 values of 2.81, 4.07 and 3.64 µM, respectively, and Ki values of 1.62, 4.10 and 2.77 µM, respectively.