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Synthesis of Anthranilic Acid Derivatives as Prolyl Endopeptidase Inhibitors

Synthesis of Anthranilic Acid Derivatives as Prolyl Endopeptidase Inhibitors

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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 $IC_{50}$ values of 2.81, 4.07 and 3.64 ${\mu}M$, respectively, and $K_i$ values of 1.62, 4.10 and 2.77 ${\mu}M$, respectively.

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