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ID: ALA1138876
Journal: Bioorg Med Chem Lett
Title: An introduction of a pyridine group into the structure of prolyl oligopeptidase inhibitors.
Authors: Jarho EM, Venäläinen JI, Juntunen J, Yli-Kokko AL, Vepsäläinen J, Christiaans JA, Forsberg MM, Järvinen T, Männistö PT, Wallén EA.
Abstract: A series of ionizable prolyl oligopeptidase inhibitors were developed through the introduction of a pyridyl group to the P3 position of the prolyl oligopeptidase inhibitor structure. The study was performed on previously developed prolyl oligopeptidase inhibitors with proline mimetics at the P2 position. The 3-pyridyl group resulted in equipotent compounds as compared to the parent compounds. It was shown that the pyridyl group improves water solubility and, in combination with a 5(R)-tert-butyl-l-prolyl group at the P2 position, good lipophilicity can be achieved.
CiteXplore: 16919454